IN THE SUPERIOR COURT FOR THE STATE OF ALASKA

THIRD JUDICIAL DISTRICT, AT ANCHORAGE

In The Matter of the Hospitalization                )

                                                                                )

                                                                of            )

                                                                                )

FAITH J. MYERS                                 )

                                                                                )               Case No. 3AN 03-277 P/S

 

STATE OF NORTH CAROLINA                      )

                                                                                ) ss

__________________ COUNTY                    )

 

 

An Analysis of  the Olanzapine Clinical Trials – Dangerous Drug,  Dubious Efficacy

 

By Grace E. Jackson, MD

March 3, 2003

 

 

 

Sources of  FDA Information:

 

Andreason, Paul.  Review and Evaluation of Clinical Data, NDA 20-592, Reviewer Completion Date: July 29, 1996, pp 1-108, Appendices 7.2.1-7.2.4, Appendix 8.

 

Andreason, Paul. Statistical Review and Evaluation, NDA 20-592, February 14, 1996.  

 

 

============================================================================

 

 

Efficacy of  Olanzapine

 

 

n       Four major studies were reviewed by the FDA for the purpose of establishing the efficacy of olanzapine in the treatment of chronic schizophrenia (acute exacerbation).  These studies

were identified with the following codes:

HGAP, HGAD, E003, HGAJ.

 

Two of these studies were rejected by the FDA and were thus omitted from the analyses

of data used in validating the efficacy of the new drug relative to placebo:

 

E003 - failed to establish any significant effectiveness for the drug in question

HGAJ - poor trial design, with unacceptable biases in favor of experimental drug

 

 

The focus of this report is a methodical analysis of the experimental biases in both the clinical trials and the FDA evaluation  process, leading to approval of the antipsychotic drug olanzapine (Zyprexa).  A specific emphasis will be placed upon the two drug trials (HGAP, HGAD) used by the FDA to corroborate efficacy and safety of the experimental drug.  These are the two trials which are referenced anonymously in the PDR and drug label.  The goal of this paper is to clarify serious problems in the clinical study designs and statistical imputations of the olanzapine trials,  so that the reader will emerge with an expanded capacity for critical reflection in psychopharmacological research and psycho-politics.

 

 

 

 

 

 


 

 

HGAP Trial

 

                Multicenter, randomized, double-blind study

                12 sites in US

Compared fixed doses of olanzapine (1.0 mg and 10.0 mg) vs. placebo

                N = 152

 

 

 

Period I     4-9 day placebo lead-in period involving 152 patients meeting DSM-IIIR criteria for   

                 schizophrenia; patients had to have initial BPRS score of at least 24 ( on scale of 0 to 6  

                 for each of the 18 items in the scale), CGI of at least 4 (moderate severity)

 

                Period II   randomization of patients into one of three treatment groups.

                                   Patients placed on olanzapine 10.0 mg were NOT titrated up to that dose from

                                   lower dose.   This phase was six weeks in duration.

 

  Subjects who had not responded to double-blind therapy after three weeks could

  enter open-label phase of study at week four.

 

   73% of subjects dropped out of study after week four.

 

   [What is NOT emphasized by the FDA or the sponsor is the fact that subjects

   were also eligible for outpatient status after week four, according to physician

   judgment.]

 

 

Period III  Period II completers (six weeks) could enter open label phase of study at visit #8 (week                       six).   Period II “changeovers  (non-responders who changed to open-label phase at

                 week four, five, or six) were allowed to continue in open label extension   

 

 

 

Concomitant medications:

 

Patients were allowed to continue a wide variety of medications which had been taken previously for

pre-existing medical conditions. Patients were  permitted to take lorezapam (Ativan) as needed or chronically, for sleep or agitation.

 

 

 


HGAP Trial

                                 

                Study Design Problems

 

1)       placebo washout: there is no  mention of  how many patients were taking neuroleptics (or other drugs) at the time of the placebo lead-in.  We do not know how many of the patients in this study were actually exhibiting symptoms of medication discontinuation.  This turns the acute phase period (upon which efficacy has been established) into a comparison of  drug withdrawal effects – withdrawal on placebo,  vs.  withdrawal on olanzapine.   The study, in effect, is a comparison of supersensitivity psychosis in three different arms of subjects.

 

2)       failure of dose titration: again, patients were abruptly placed on 10.0 mg of Zyprexa in one arm of this study.  This may have prejudiced results for that group in a favorable direction, as 10.0 mg may have had superior effects in protecting against withdrawal symptoms in those patients who had previously been taking neuroleptics for an extended period of time, or in subjects who may have been given high doses of potent drugs acutely.

 

 

3)       concomitant medications:  the allowance of  concomitant medications for pre-existing medical conditions was an understandable part of the trial.  However, it is unclear that the FDA or the drug sponsor has given adequate consideration to the impact of this variable.  Concomitant medications given for pre-existing medical problems may be confounding factors in the trial for three reasons:

a)       many of the drugs permitted are known to have significant effects upon the brain (e.g.,  antihistamines, hormones, antihypertensives, cough medicines, and H2 blockers);

b)       many of the permitted drugs are known to induce or inhibit liver enzymes responsible for the metabolism of the experimental drug;

 

and

 

c)       many of the pre-existing medical conditions for which concomitant drugs were allowed are, themselves, known risk factors for many of the symptoms which the trial was designed to track.

 

 

The use of lorazepam was allowed for acute or chronic insomnia or agitation.  However, the FDA data do not present sufficient information to know which subjects were given lorazepam in each of the study arms, nor can it be determined to what degree the use of this drug may have contributed to patient outcomes according to responders and drop-outs.

The FDA database makes no reference to information which would permit a reasonable analysis of subject endpoints, based upon the possibility that “lack of efficacy” occurred in a

higher proportion of those subjects who were not given lorazepam for neuroleptic-induced anxiety, neuroleptic withdrawal, or their pre-existing condition.

While Andreason contends that “there were no significant differences in the use of concomitant medications between groups” (meaning: olanzapine vs. placebo),  this does not settle the question of the extent to which lorazepam use varied between RESPONDERS and COMPLETERS.

 


HGAP Trial

 

Study Design Problems

 

4)       Drop-out rate:  Period II  was the “efficacy period,” intended to last six weeks. 

Only 27% of  the subjects completed Period II.   This turned the HGAP study into a FOUR WEEK study.   No results obtained after the four week mark can be generalized to the larger population, but results obtained at the six week mark are still interesting, as they demonstrate  how closely placebo completers and olanzapine completers resembled each other in terms of SYMPTOM severity.

 

The implication is that there was NO DIFFERENCE between olanzapine and placebo in those who continued treatment.

 

 

===============================================================

** Results obtained AFTER the four-week mark cannot be used for the purpose of generalization to the larger population,  as the study is underpowered (not enough subjects)  to meet statistical  requirements   [80% power,  > or = 40% reduction in BPRS scores,

assumption of standard deviation = 14.56].

 

 

To find size needed to treat (past week four)

Take standardized effect size = desired mean change on BPRS  /  standard deviation 

then locate sample size for that standardized ES at 80% power:

 

                       standardized effect size = 10 / 14.56   =    0.68

                     for 80% power (B = 0.20, alpha = 0.05),   sample size  =  26 in each arm

                      None of the treatment arms had 26 subjects or more past week four.

 

 

5)       Reasons for the large drop-outs across all treatment groups after week FOUR

 

(Statistical Review and Evaluation, pp1-3)

 

 

Andreason acknowledges in his Statistical Review and Evaluation that  physicians were free 

to qualify subjects for open-label participation at the four-week mark of the study, based upon “patient performance …and physician judgment.”  The FDA was appropriately concerned about the cause(s) of  the 73% drop-out rate after four weeks.  When queried, the sponsor’s representative (Dr. Charles Beasley)  stated that many investigators had worried about the study design, in which they presumed that 2/3 of the subjects would invariably be harmed (greater risk of relapse) by treatment with placebo, or a dose of olanzapine believed to be non-active (ersatz placebo). 

 

According to Beasley, subjects were disenrolled from the study at week four in order to spare them the “possibility of being continued in a group which investigators believed would be more prone to relapse.”   This makes little sense, based upon a trial design process which permitted physicians to transfer non-responders into the open label phase after week three.

 

Also, numerically speaking,  20 of the olanzapine 10 mg subjects dropped out of the study after week four, but we do not know how many of these subjects did so because of  side effects or lack of efficacy.  Given the large number of drop-outs occurring even within the assumed “effective” treatment arm, one must consider additional reasons for the poor completion rate in this study.

  

 

HGAP Trial

 

 

Study Design Problems

 

 

One potential source of experimental bias, apparently neglected by the FDA,

is the fact that patients first became eligible for conversion to outpatient status based upon their week four assessment.  This suggests (although by no means confirms) a bias in the study, whereby patients desirous of discharge  from the hospital may have inflated their answers on rating instruments at weeks five and six.

 

As the data that are reported  do not distinguish endpoints on the basis of  “inpatient”  vs.  outpatient  reporting in weeks five and six, we cannot determine the extent to which patient “improvement” may have been compromised by a patient’s  overriding desire to obtain or continue outpatient status.  Similarly, we cannot know the extent to which physicians themselves were influenced (consciously or otherwise) in their assessments of subjects, due to the possible impact of such ratings upon treatment locale.

 


 

HGAP

 

Efficacy Results

 

 

 

1) “Dropouts were OVERWHELMING” (Andreason, Statistical Review and Evaluation pg 2).

 

2) Completers in the placebo and olanzapine arms “not only did not differ at the end of the trial, but also hardly varied from each other during the whole course of the trial.”  (Andreason, Statistical  Review p2)

 

 

3) Percentage of  Responders:

 

Responders were those subjects who demonstrated a change in BPRS of  40% or more, following  a minimum completion of two weeks in the study

 

                        Responders

 

        Placebo arm                   4/ 43 subjects  =  9.5%

       Olanzapine 10.0 mg      12/42 subjects  = 27.9%

 

 

4) Comparison of the average slopes for BPRS over time (a form of repeated measures analysis,  

considered by many statisticians to be superior to LOCF)  demonstrated NO statistical significance between treatment groups (p =.345).

 

 

5) Re: possibility that negative symptoms caused by neuroleptics or neuroleptic withdrawal confounded endpoints

 

The  FDA report  (Statistical and Evaluation Review, pg 3) reveals  that the sponsor performed a covariate analysis for the negative PANSS, using as covariates the changes from baseline in positive PANSS,

PANSS depression item, and parkinsonian symptoms (Simpson-Angus Scale total).   The FDA does not supply these data.  However, the FDA states that this analysis demonstrated “no statistical differences” in any arm.  This failure to obtain statistical significance may have been a reflection of the poor study power, due to high drop-out rates.  It would be especially important for the FDA to confirm the extent to which parkinsonian symptoms may have confounded efficacy and drop-out rates in both placebo and experimental drug groups.

 

6) LOCF vs. OC data:

 

Endpoint data (efficacy results)  were collected by assessing scores on several rating scales commonly used by RESEARCHERS (but not by everyday clinicians) to assess psychotic symptoms.   Results were reported in two ways: 

 

                LOCF =  last observation carried forward

wherever a subject dropped out of the study, the last measured score was used as the endpoint for that individual.

 

                                OC = observed cases

                                wherever a subject remained in the study (27% at end of six weeks), the most current

                                rating was used as the endpoint

 

 

HGAP Trial

 

Efficacy Results

 

 

6) LOCF vs. OC data:

 

The FDA concedes that “OC data at week six did not support olanzapine as being effective

(Review and Evaluation of Clinical Data, p17).   

 

Dr. Andreason is apologetic for this finding, but then sides with the manufacturer by suggesting that Observed Case data should be dismissed.  Per Andreason, “OC data reflect the high drop-out rate of placebo treated patients who could not remain in the study… this left the least symptomatic patients in all groups to compare against each other.   It is for this reason that LOCF and not OC data represent a clearer picture of the true efficacy of olanzapine in this patient population.” 

[Review and Evaluation of Clinical Data,  p 18 ]

 

In fact, at the six week mark of the study, almost EQUAL numbers of subjects remained in EACH group – particularly if the placebo pool  is combined with the olanzapine 1.0 mg pool:

                                               

                                Subjects Remaining at Six Weeks

 

 

Placebo                                  N = 50       at six weeks:  N = 10   20%

                                Olanzapine 1.0 mg                N = 32         at six weeks:  N = 12   23%

                                Olanzapine 10.0 mg              N = 50         at six weeks:  N = 19   38%

 

 

                Thus, at the end of  the six week acute phase, OC data demonstrate a comparison

                between 22 subjects taking either placebo or the lowest dose of olanzapine,

                and 19 subjects taking 10.0 mg of olanzapine.

                This suggests that OC data provide a very good gauge of six-week outcomes,

                for those subjects willing or able to remain in the study for the full six weeks.

If Andreason wants to suggest that six-week data unfairly reflect “less symptomatic placebo subjects” due to previous drop-outs,  then he must logically concede that six-week data similarly reflect “less symptomatic olanzapine subjects” due to previous drop-outs.

 

 

 


HGAP Trial

 

 

Efficacy Results

 

                                Andreason contends that LOCF gives a truer picture of medication efficacy.

                                What LOCF PROBABLY gives is a truer picture of  how the active forms of  any

                                drug (compared to placebo) are able to eclipse drug withdrawal or rebound symptoms

                             in study subjects, as we can assume that most of these individuals were abruptly removed

from their previous medication regimens during the placebo lead- in

                             phase.

 

                                Andreason implies that placebo patients “left the study” in a disproportionate fashion

due to lack of efficacy.  In fact, the number of patients who left the study for “lack of

efficacy  was impressive BUT NOT STATISTICALLY significant across  all three

groups of subjects:

 

 

                                HGAP drop-outs due to lack of efficacy

 

                74%                     of   placebo patients

                62 %                    of  1.0 mg olanzapine patients

                56%                      of 10.0 mg olanzapine patients

                                               

 

 

A final concern about “efficacy” as measured by the FDA in all of the trials pertains to effect size.   This means that statistics are presented, and conclusions drawn, relative to reductions in symptoms on the BPRS, PANSS (positive and negative), or CGI rating scales.  What is not emphasized by Dr. Andreason (FDA) is the fact that there is much debate about the meaning of these changes in scores.  Thus, while statistically significant differences in rating scales may be obtained across studies, there is no consensus that any of these observed differences are of  CLINICAL import (that is to say, a change of  5 points might be just as clinically meaningful, or meaningless, as a change of 10-20 points).  The FDA

side-steps this very important philosophical and clinical issue,  although Dr. Paul Leber is at least decent enough to mention this problem in a memo addressed to Dr. Robert Temple on  AUG 18 1996.  It is also possible that many patients experience a  temporary regression as a part of  recovery from an acute psychotic episode.  To the extent that this results in changes in rating scales, there may be a false assumption that early reductions in symptoms portend the best long-term prognosis.

 

 

·         Note:  BOTH of these interpretive problems  occur throughout the FDA analysis of the olanzapine trials:

 

1)  preference for LOCF  data  instead of OC data to establish efficacy

2) acceptance of  statistically significant  “mean changes” (on rating scales) despite lack of

            evidence that these measures are in any way clinically meaningful

 

 

 

 


 

 

HGAD Trial

 

                Multicenter, randomized, double blind study

                23 sites in US and Canada

                Compared multiple fixed doses of olanzapine (5.0 mg +/- 2.5, 10 mg +/- 2.5, 15 mg +/- 2.5)

                against ONE fixed dose of Haldol (15.0 mg +/- 5.0 mg) and placebo.

 

                N = 335

 

Period I     4-9 day placebo lead-in period (neuroleptic washout) involving 419 inpatients meeting   

                 DSM-IIIR criteria for schizophrenia (experiencing acute exacerbation of their illness:

                 initial BPRS score of at least 24 and CGI of at least four)

 

                  Note: 84 patients were not continued in the study.  Reasons are not given in the FDA

                  record, but these drop-outs may have been due to unfavorably high rate of placebo 

                response in some of these subjects (i.e., investigators elected not to continue individuals

                 who demonstrated too much improvement in BPRS while taking placebo during the  

               lead-in phase).

 

                Period II   Randomization of  335 patients into one of three treatment groups for six weeks

                                   (multiple dose olanzapine, fixed dose Haldol, placebo).

   At visit #5 (week two), subjects could switch over to open-label arm as

   OUTPATIENTS depending upon performance in trial and physician judgment.                                 

                Period III   continuation of double blind for up to one year in subjects who were positive

                                 responders in period II. 

 

                Period IV  open ended continuation of  period III in subjects who wanted to continue

                                 in double blind therapy

                                   

 

                Period V      open label extension for patients who had previous exposure to olanzapine

                                     who wanted to continue 

                                  

·         Note: principal investigator at study site #2 (Dr. Richard L. Borison) was indicted

for research misconduct.  While FDA dismisses the relative importance of Borison’s data (number of patients contributed to database = 17),  the results from his center were nonetheless reviewed and included for the purposes of determining olanzapine’s efficacy.

 

Concomitant medications:

 

Patients were allowed to continue a wide variety of medications which had been taken previously for

pre-existing medical conditions. Patients were  permitted to take lorezapam (Ativan) as needed or chronically, for sleep or agitation.

 

 

 

 

 

 


 

 

HGAD Trial

 

 

Problems in Study Design

                               

1)       placebo washout and abrupt neuroleptic withdrawal syndromes:

there is no  mention of  how many patients were taking neuroleptics (or other drugs) immediately prior to the  placebo lead-in phase, but it is presumed that this number was

high (all patients were inpatients at the start of  the study, experiencing an exacerbation of symptoms).

 

Thus, we can assume that many of the subjects randomized to the placebo or low dose olanzapine arms of the study manifested the symptoms of neuroleptic WITHDRAWAL

in addition to, or instead of,  symptoms of their pre-existing  schizophrenia.  [ In fact, we do not know how many of these same subjects were experiencing the “exacerbation” of their psychoses because of an earlier withdrawal from neuroleptics.  In that case,  the trial

simply extended or repeated those previous experiences.]   Thus, the trial was designed in such a way as to induce, or worsen, symptoms of schizophrenia in the study groups who were not exposed to the experimental drug at medium or higher doses.

                      HGAD is a clinical trial that compares neuroleptic withdrawal syndromes (supersensitivity

                      psychosis  and/or  tardive phenomena) in  three different arms of subjects.

 

                     

2)       placebo lead-in and removal of early placebo responders:  419 subjects were enrolled in the study, based upon selection criteria.   84 of these subjects were disrenrolled during the first 4-9 days of the study.  No reasons are given by the FDA for this large drop-out, but one can assume that these subjects were removed from the study in order to maxmize comparative

efficacy of the experimental drug.   In other words, subjects who responded to placebo

early in the study were simply not counted in the final results, so that the overall pool of placebo responders was reduced.

 

3)       Comparison of non-equieffective doses:

Patients on olanzapine were given doses ranging from 5.0 mg (+/- 2.5 mg)  up to 15 mg (+/- 2.5 mg).  Patients on haloperidol were given a fixed dose in range of 15.0 mg (+/- 5.0 mg).

 

In terms of  BINDING affinity, the comparative doses for each level of olanzapine used

in this study would have been as follows:

 

(This information is taken from Bezchlibnyk-Butler and Jeffries (2002),

Clinical Handbook of Psychotropic Drugs, Seattle: Hogrefe & Huber Publishers,

pp 90-91)

 

olanzapine 10 mg (based on D2 affinity and pharmacokinetics)

                                  55-80% D2 Receptor occupancy

 

 

haloperidol   2 mg  (based on D2 affinity and pharmacokinetics)

                                   75-89% of D2 Receptor occupancy

 

 


 

HGAD Trial

 

 

 

Study Design Problems

 

 

4) Non-equieffective Doses

 

 

In terms of receptor binding and D2 occupancy, 10 mg of olanzapine would have been

equieffectively dosed with 2 mg of haloperidol.

 

In THIS study (as in all the other studies with Haldol), we see the following comparisons:

Olanzapine  2.5 mg – 7.5 mg          vs.     Haldol  10 – 20 mg

Olanzapine   7.5 – 12.5 mg              vs.    Haldol  10 – 20 mg

Olanzapine   12.5 – 17.5 mg            vs.    Haldol  10 – 20 mg

 

Equieffective DOSING would have been:

 

Olanzapine  2.5 – 7.5 mg                  vs.  Haldol      0.5mg  - 2.5 mg

Olanzapine 7.5 mg – 12.5 mg       vs.  Haldol      1.5 mg – 2.5 mg

Olanzapine 12.5 mg – 17.5 mg     vs.  Haldol      2.5 mg – 3.5 mg

 

 

 

This means that patients in olanzapine HIGH arm of study received 4-6 TIMES the equivalent

dose of Haldol ( OVERDOSED on HALDOL  four- to  six-fold).   Patients in olanzapine

MEDIUM arm received 7-8 TIMES the equivalent dose of  Haldol (overdosed on Haldol

 seven- to eight-fold).   Patients in olanzapine LOW arm of study received 8 to 20 times

the equieffective dose of Haldol (OVERDOSED eight- to TWENTYfold).

This HAD to have prejudiced DROPOUT from study in favor of olanzapine, due to side effects or

lack of efficacy.

 

Why OVER-DOSING Haldol contributes to DIMINISHED efficacy on Rating Scales Used in the Study

 

Due to the use of such high levels of a potent, typical neuroleptic (Haldol), it is likely that Haldol

subjects experienced more parkinsonian symptoms (and possibly more TD) than olanzapine subjects. 

This would necessarily contribute to elevations in negative symptoms of schizophrenia, reflected in both total BPRS scores,  PANSS (negative), and CGI.   There is a substantial body of literature documenting the phenomena of NEUROLEPTIC INDUCED DEFICITS, Tardive Dysmentia, and Tardive Anosognosia.  

 

Without testing specifically for the variance in negative symptoms associated with EPS or TD in  the olanzapine vs. Haldol subjects, the FDA cannot conclude that olanzapine has superior efficacy (compared to Haldol) in treating schizophrenia.   Eli Lilly has unfairly prejudiced the outcome results by INDUCING or EXACERBATING pre-existing negative symptoms  in Haldol subjects,  while giving comparatively low doses (D2 receptor occupancy) in the olanzapine subjects. 

 

It is important to remember that negative parkinsonian symptoms seem to be linked closely to D2 receptor blockade; thus, it is significant that the study compares 55-80% receptor occupancy in olanzapine against 75-89% receptor occupancy in haloperidol.   One must wonder what kinds of EPS or TD might emerge in olanzapine patients maintained on doses that result in 75-89% receptor occupancy.

 

[ SEE references on  NIDS, Tardive Dysmentia, Tardive Frontal Lobe Syndromes ]

 

 

HGAD Trial

 

 

Study Design Problems

 

 

 

5) Drop-out: Only 42% of 335 subjects completed six weeks of this study.

 

Andreason (Statistical Review and Evaluation, pg 3) concedes: “Dropouts were overwhelming due to lack of efficacy.

 

 

 

HGAD Completion Rates (at six weeks) were as follows:

 

Placebo                                  N = 22       32.4%

olanzapine low                      N = 27       41.5%

olanzapine    med                  N = 26       40.6%

olanzapine  high                 N = 34       49.3%

Haldol                                    N = 30       43.5%         

 

 

HGAD Drop-Out Rates

 

                                Lack of Efficacy                    Adverse Event                     Patient Decision

Placebo                  N = 32      47%                       N = 7   10.3%                         N = 2      2.9%

Olz low                   N = 22        33.8%                  N = 5     7.7%                         N = 7       10.8%

Olz med                  N = 24      37.5%                    N = 1       1.6%                       N = 7       10.9%

Olz high                 N = 18      26.1%                    N = 4      5.8%                        N = 7     10.1%

Haldol                    N = 19        27.5%                  N = 6      8.7%                        N = 7     10.1%

 

 

RE:  Drop-out for lack of efficacy:

 

Placebo patients dropped out more frequently for lack of efficacy than olanzapine and Haldol, but this is what one would expect given the fact that these were patients in the midst of placebo-washout from previous neuroleptics (all patients had been in hospital for at least 4-9 days, presumably on neuroleptics and/or other drugs).

 

 

RE: Drop-out for adverse events:

 

Adverse events were higher in the placebo and Haldol patients.  Placebo events may have been attributable to neuroleptic withdrawal.  Haldol events may have been attributable to non-equieffective (HIGH) doses used for that arm of the study.

 

 

RE: Drop-out for “patient decision”:

·         Note: no discussion or clarification is offered to explain the content of these patient decisions,

but it is reasonable to suspect that withdrawal syndromes in the placebo arm, and  side effects

 in the active drug arms (especially weight gain or sedation in olanzapine; akathisia, EPS, and/or TD in Haldol) may have been contributing factors.

 


 

HGAD Trial

 

Study Design Problems

 

 

6) cross-over to outpatient status: investigators were permitted to switch subjects into the OPEN label   

    OUTPATIENT phase of the study after two weeks of observation.    This decision removed the    

    double blind” of the investigation at a very early point in the trial.  In effect, this was NOT a

    double-blinded study after two weeks (if it ever was).   Furthermore, it is highly likely that outpatient

    status – once attained – was not likely to be jeopardized by patients who might otherwise have

    communicated more openly about deterioration or plateau in symptoms.    The decision to permit

    olanzapine patients to continue their medications in a non-blinded, outpatient status after TWO weeks

    may have substantially favored outcomes for the experimental drug.

 

 


 

HGAD Trial

 

Efficacy Results

 

 

1)       BPRS baselines used in this study were slightly higher in olanzapine subjects than in Haldol or placebo subjects.  That is to say,  the study examined multiple fixed doses of olanzapine in a “sicker” group of patients at the start of the study.  This may have made it easier to demonstrate larger RELATIVE improvements  in olanzapine patients (vs. placebo).

 

2)       No dose effect was revealed in this study.  Olanzapine-MED showed improvement over placebo

in Observed Case BPRS positive scale, but NOT in BPRS negative scale.  In general, Observed Case

data failed to prove that olanzapine is more effective than placebo.

 

3)    No endpoints in  the Observed Case  SANS  or  CGI Severity scales attained statistical significance.

       BPRS total score change in Observed Cases did attain statistical significance in olanzapine medium

       and olanzapine high (relative to placebo), but the clinical significance of these changes is uncertain.

       That is to say, it is unclear that a mean change in total BPRS of  ten is clinically more meaningful than

       a mean change of  five.

 

4)   Dr. Andreason again gives preference to LOCF data, suggesting that OC data reflect “less

      symptomatic placebo subjects.”   Andreason implies that Observed Case data are invalid because they

      reflect  the symptom level of a subject pool that remains following  a large number of drop-outs for

      low efficacy.  In fact, the statistics demonstrate that LACK OF EFFICACY was a common

      occurrence  across all arms of the trial.   

 

The FDA decision to validate olanzapine efficacy using LOCF methodology compels a closer consideration of the limitations of this approach:

 

a)       LOCF improperly assumes that all subjects who drop out will

remain stable (i.e., last observed endpoint will neither improve, nor deteriorate)

                       This is an especially dangerous assumption to make in psychiatry, where many

                       conditions may actually improve over time

 

 

b)       LOCF artificially inflates the advantages of the experimental DRUG by assuming that placebo (or comparison drug) drop-outs are occurring primarily for lack of efficacy.  However, it is just as likely that placebo or comparison drug subjects drop out because of intolerable side effects associated with the respective treatment conditions (in other words, placebo subjects may drop out because of  symptoms of neuroleptic withdrawal, rather

than  schizophrenia

 

c)       LOCF fails to make appropriate use of ALL data points BEFORE the last visit.

By simply taking the last available data point, and by projecting it forward in time,

LOCF loses the trajectory of how each subject may have been improving or deteriorating

over time.


HGAD Trial

 

Efficacy Results

 

5)   Responder analysis demonstrates that there was NO statistically significant difference between  

       the PROPORTION of subjects in each arm of the study who RESPONDED to treatment, for purpose

       of any pairwise comparison.

 

                Olanzapine High     32/65  subjects  or     49.2%  responded

                Placebo                    21/62   subjects  or    33.9%  responded

 

 

 


 

E003 Trial

 

                Not used for efficacy evaluation due to negative findings

              No placebo arm.    

                Providers allowed to tritate doses up/down farily liberally for clinical effect.

 

                Highlights of this study

                Multicenter, randomized, double blind study

                50 sites in Europe, South Africa, Australia, Israel

                431 patients.

               

                Compared several fixed dose RANGES of olanzapine (5.0 mg, 10.0 mg, 15.0 mg  +/- 2.5) vs.

                Fixed dose olanzapine (1.0 mg)  vs. fixed dose RANGE of Haldol (15.0 mg +/- 5.0)

  

Only 47% of the subjects completed six weeks.

 

*No significant improvement was noted in olanzapine (low / medium / high) doses vs.  Haldol  or   “homeopathic”  fixed dose of  Olanzapine (1.0 mg).

               

 

FDA was at a loss as to what they should do with this study, which suggested that 1.0 mg of olanzapine was having  a beneficial effect in a significant number of  patients.    Andreason called this a “failed study” but did not explain what he meant by the word:  failed.  For thoughtful students of  placebo effects, this study was a marked VICTORY.

 

It appears that the FDA buried this study, out of embarrassment or panic that it showed NO dose effect; and worse, it implied that 1.0 mg of olanzapine was inducing a placebo benefit in patients.  After all,

if   a  1.0 mg dose of olanzapine could produce benefits (“active” placebo ?) ,  then clinicians might have to consider the possibility that 2.5 mg, 5 mg, or 10 mg doses  might also exert their salutary effects through placebo mechanisms in the body,  rather than D2 receptor occupancy.

 

               


 

HGAJ Trial

 

                Not used for efficacy evaluation  due to poor design

                Multicenter, randomized, double blind

                186 sites in US and Europe

                N = 1996 patients

                Compared olanzapine RANGE (5 – 20 mg) vs. Haldol range (5 – 20 mg).

                NO placebo arm.

                Broader inclusion criteria: schizophrenia, schizophreniform, and schizoaffective.

Included subjects who had experienced adverse event on recent or current neuroleptic, or

               subjects who were “not tolerating their pre-study treatments.”

 

 

FDA DECLINED to use this study for efficacy (but did use it for safety database),  due to problems

with selection bias.   38% of Haldol patients enrolled in study had FAILED Haldol previously.

 

In discussing the HGAJ study, Andreason expresses for the first time some concerns about:

 

 

a)       “non-comparable dose ranges”

 

without elaborating, Andreason suggests that dosing the two drugs on a “mg. for mg basis”

                        biased the study “against Haldol.”  He suggested that dosing at lower doses, or slower dose

                        increases would have similarly disfavored olanzapine (Review and Evaluation of Clinical

                        Data, p. 33)

 

b)       rating scale results (mean rating scores): Andreason raises for the first time

some concerns that difference in mean scores had attained statistical

significance,  but  that this significance (of dubious clinical significance – see pg 33)

had been reached  only after  increasing the size of  the study to very large  numbers.

He concludes that the study was OVERPOWERED, in order to obtain statistical

significance on the rating scales

 

 

While it is encouraging that Andreason finally acknowledges some of these problems in the HGAJ study,

it is worrisome that he is not similarly able to apply the same limitations to the two studies (HGAP, HGAD) whose data were used to establish the efficacy of the experimental drug. [ i.e.,  HGAD also suffered from non-comparable dose ranges; HGAD and HGAP both suffered from rating scales whose clinical significance remains dubious]

 

 

 

 

 


 

 

 

Summary – Problems in Olanzapine Clinical Trials

 

Study Design and Efficacy Results

 

 

 

1)       No mention of previous drugs taken by patients in all arms of studies.

 

We do not know how many drugs were being consumed by subjects before or during the trials.

We do not know to what extent symptoms tracked during the studies were manifestations of an underlying condition, rather than manifestations of neuroleptic induced deficits or neuroleptic discontinuation syndromes.

 

2)       Failure to maintain “double blind”.

 

A number of the studies used for the purposes of establishing clnical efficacy broke the double blind intentionally, by permitting investigators to remove subjects into the open phase of the study.   It is also possible that the “blinded” nature of the studies was further compromised by the adverse reactions present in many patients who received active neuroleptics (for example: weight gain and sedation with olanzapine; akathisia with Haldol).

      

 

3)       Concomitant medications:

 

Despite the efforts of investigators to limit the use of centrally active medications in these studies, it appears that patients were permitted to continue using a wide variety of chemicals with known neuropsychiatric effects.   These include hormonal therapies, antihypertensives, and H2 blockers.   No data appear in the FDA report to explain treatment differences in subject arms according to the use of “permitted” concomitant medications.  As lorazepam (Ativan) was allowed in many studies for the treatment of anxiety and insomnia, it would be important to know how many placebo vs. olanzapine subjects had endpoints which were influenced by the use of the benzodiazepine. 

 

4)       High drop-out rates:

 

HGAP  73%      drop-out rate in four weeks

HGAD 68%      drop-out rate in six weeks

 

Even the FDA analysts themselves refer on numerous occasions to the “overwhelming drop-out rates” present in the olanzapine studies.  The loss of so many subjects presents two problems: first, it prevents the generalization of findings to a larger population.  Second, it creates methodological problems in the evaluation of treatment differences.  (see below)

 

Based upon these drop-out rates in the acute phases of the studies, the FDA appropriately refused to approve olanzapine as a maintenance therapy for schizophrenia, arguing that its long term effectiveness had not been demonstrated.


 

Summary of Problems – Study Design / Efficacy

 

 

 

5)       Placebo Washout:

 

In one study (HGAD), the FDA refused to address the large number of drop-outs (84) which occurred in the first four to nine days of the study.  As this was the placebo “lead-in” phase of  the study, it is possible that these 84 individuals were removed because they demonstrated an unacceptably favorable response to the early placebo treatment.  By removing these 84 subjects from the overall data pool, the investigators biased the results in favor of the experimental drug (removing the placebo responders necessarily raised the comparative efficacy of olanzapine – particularly in LOCF analysis).

 

 

6)       LOCF (last observation carried forward) to validate efficacy:

 

In order to compensate for the missing data created by large numbers of drop-outs, the FDA used the LOCF technique.   This method involved taking  the last observed clinical findings in each subject

who disenrolled,  then carrying those ratings forward to each successive evaluation period as though each subject in question had NOT CHANGED over time. 

 

LOCF data fail to capture the possible improvement of subjects, who might be lost to follow-up or who might withdraw from a study when they are feeling improved.  LOCF data also assume that drop-outs occur primarily f