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PFIZER INC.

These results are supplied for informational purposes only.

Prescribing decisions should be made based on the approved package insert.

For publications based on this study, see associated bibliography.



PROPRIETARY DRUG NAME/INN: Lyrica®/Pregabalin



THERAPEUTIC AREA AND FDA APPROVED INDICATIONS: See USPI.



PROTOCOL NO.: 1008-155



PROTOCOL TITLE: A 12-Week, Randomized, Double-Blind, Multicenter, Placebo-

Controlled Study of Pregabalin Using an Individual Optimal Twice a Day (BID) Dose Schedule

in Patients With Chronic Neuropathic Pain



Study Center(s): Sixty in Austria, France, Germany, Switzerland, Poland, Spain, Portugal, The

Netherlands, and The United Kingdom



Study Initiation and Completion Dates: 04 July 2001 to 23 December 2002



Phase of Development: Phase 3



Study Objective(s): To evaluate the efficacy, safety, and tolerability of 2 pregabalin treatments

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









(600 mg/day fixed dose; 150-600 mg/day titration) to placebo for pain relief in patients with

neuropathic pain



METHODS

Study Design: Following a 1-week Baseline phase, study medication was administered orally

BID in a double-blinded fashion for 12 weeks as pregabalin capsules or matching placebo if

inclusion criteria were met. Qualified patients were randomized to 1 of 3 orally administrated

BID double-blinded treatment groups:

• Escalating doses of pregabalin 150, 300, 450, and 600 mg/day titrated in weekly

intervals based on patients’ individual responses and toleration of treatment

• Pregabalin 600 mg/day, starting with pregabalin 300 mg/day for 1 week: the target

dose of pregabalin 600 mg/day remained stable from the end of Week 1 onwards as a

fixed dose for 11 weeks

• Placebo for the 12-week treatment: the randomization schedule was 1:2:2, placebo,

pregabalin fixed dose, and pregabalin flexible dose, respectively. At the end of the

double-blind phase or at the time of early termination by the patient, medication was

either continued in an open-label, follow-on study (Protocol 1008-166) or

discontinued



Number of Patients (planned and analyzed):

Planned: Three hundred and twenty-five (325) patients



Analyzed: Five hundred and three (503) patients were screened; 338 patients were randomized

and treated.

CLINICAL STUDY SYNOPSIS



Diagnosis and Main Criteria for Inclusion: Men or nonpregnant, nonlactating women ≥18

years of age were included in the study. Postherpetic neuralgia (PHN) patients must have had

pain present for more than 3 months after healing of the herpes zoster skin rash. Diabetic

peripheral neuropathy (DPN) patients with diabetes mellitus (type 1 or 2) who had symptoms of

pain associated with painful, distal, symmetrical, sensorimotor polyneuropathy due to diabetes

for at least 6 months, and hemoglobin A1c levels of ≤11% were eligible to enter the study.

Patients at Baseline (V1) were required to have a score ≥40 mm on the Visual Analogue Scale

(VAS) of the Short-Form McGill Pain Questionnaire (SF-MPQ). At randomization (V2), patients

had to have completed at least 4 daily pain diaries (pain was assessed daily upon awakening and

recorded in a diary), have a score ≥40 mm on the VAS of the SF-MPQ, and an average daily

pain score ≥4 over the last 7 days on the daily pain diary.



Study Treatment: Pregabalin 75 mg, 150 mg and 300 mg capsules, or matched placebo, for

oral administration for a duration of 12 weeks



Efficacy Evaluations:

Primary: The endpoint was mean pain score taken from the patients’ daily pain diaries.

Supplemental analyses of the daily pain diary data included a comparison of the proportion of

responders and repeated measures analysis of the weekly mean pain scores.



Secondary: Sensory, affective, and total scores, present pain intensity (PPI) index and the VAS

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









score from the SF-MPQ; the Daily Sleep Interference Diary; the Medical Outcomes Study

(MOS)-Sleep Scale; the Patient Global Impression of Change (PGIC), the Short-Form 36 Health

Survey (SF-36); the EuroQOL Health Utilities Index (EQ-5D); and signs/symptoms of allodynia

and hyperalgesia were secondary endpoints.



Safety Evaluations: All patients who had taken at least 1 dose of study medication (safety

population) were included in the evaluation of safety. Patients were observed and queried in a

nonspecific fashion at each visit for new or continuing adverse events. Safety evaluations were

based on adverse events; physical and neurological examinations (including peripheral sensory

examinations for DPN patients); 12-lead electrocardiogram (ECG); edema and weight

assessments and vital signs; and clinical laboratory tests (including hematology, blood chemistry,

serum pregnancy tests [female patients of childbearing potential], and urinalysis). Adverse

events were monitored throughout the study and examined by nature, intensity, and relationship

to treatment.



Statistical Methods:

Efficacy: Primary and secondary efficacy analyses were performed using data from the Intent-to-

Treat (ITT) population, defined as all randomized patients who received at least 1 dose of study

medication and who had at least 1 post-baseline efficacy evaluation. All statistical analysis

testing was 2-sided and performed at the 0.05 level. The Hochberg procedure was used to adjust

the significance level for multiplicity in statistical inference for a given efficacy parameter.

Endpoint mean pain scores; SF-MPQ total, sensory, and affective scores; VAS; PPI indices;

mean sleep interference scores; EQ-5D; SF-36 domains; and MOS-Sleep Scale (6 sleep scales

and overall problem index) were analyzed using an analysis of covariance (ANCOVA).

Proportion of responders and MOS-Sleep Scale optimal sleep scores were analyzed using a



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CLINICAL STUDY SYNOPSIS



logistic regression model. PGIC, allodynia, and hyperalgesia were analyzed using the Cochran-

Mantel-Haenzel procedure with modified ridit scores. A supplemental repeated measures

analysis of mean pain scores and weekly mean sleep interference scores was also carried out.

Percentages of patients with sign/symptoms of allodynia and hyperalgesia at Baseline and

endpoint were calculated.



Safety: All patients randomized who had taken at least 1 dose of study medication were included

in the evaluation of safety, which was carried out using descriptive statistical methods. For

summarization of adverse events, the investigator’s terms for individual adverse events were

mapped to preferred terms using Coding Symbols for a Thesaurus of Adverse Reaction Terms

(COSTART) IV. Associated adverse events were also summarized and included those events the

investigator considered possibly, probably, or definitely related to the study medication, as well

as those for which the relationship was unknown. Time to onset and duration of adverse events

were also computed. In evaluations of clinical laboratory parameters, the last determinations

obtained before study drug was initiated served as Baseline value. Patients were categorized

according to whether their values were below, within, or above normal range at Baseline and at

the final determination. For each parameter, matrix tables display the number and percent of

patients in each treatment group with values changing categories or remaining stable at

termination as compared with Baseline.



RESULTS

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Subject Disposition and Demography: A total of 503 patients were screened; 338 patients

were randomized and treated and 209 subjects patients completed the study. Overall, 30/65

(46.2%) patients in the placebo group, 49/141 (34.8%) patients in the pregabalin flexible dose

group, and 50/132 (37.9%) patients in the pregabalin fixed dose treatment group withdrew

during the treatment phase of the study. The most common reason for withdrawal of patients in

the placebo group was lack of efficacy (19 [29.2%] patients compared with 12 [8.5%] patients in

the pregabalin flexible dose treatment group and 11 [8.3%] patients in the pregabalin fixed dose

treatment group). The most common reason for withdrawal among patients treated with

pregabalin was adverse events (24 [17.0%] patients in the pregabalin flexible dose treatment

group and 33 [25.0%] patients in the pregabalin fixed dose treatment group versus 5 [7.7%]

patients in the placebo group). The study included 89 (26.3%) patients with PHN and 249

(73.7%) patients with DPN.



The majority of patients were white (97.6%), male (54.1%), and between 18 and 64 years of age

(52.4%). The mean age was 62.2 years, with a range of 26 to 87 years. The mean estimated

Baseline CLcr was 88.1 mL/min for all patients with a range of 46.0 to 178.0 mL/min.

Demographic characteristics were similar across the 3 treatment groups.



Efficacy Results: Primary: The results of the comparison of the primary efficacy parameter of

endpoint mean pain scores based on the patient’s daily diary data are presented in Table S1.









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CLINICAL STUDY SYNOPSIS



Table S1 Endpointa Mean Pain Scores: Results of ANCOVA (ITT Population)

Treatment N Least Squares Treatment Comparisons (Placebo - Pregabalin)

Mean SE Difference 95% CI Unadjusted Adjustedb P-

P-Value Value

Placebo 62 4.983 0.321

PGB Flexible Dose 139 3.809 0.230 1.174 (0.452, 1.897) 0.002 0.002

PGB Fixed Dose 128 3.602 0.239 1.380 (0.647, 2.113) <0.001 <0.001

Interactions:

• Treatment by Center (Generalizability), p = 0.495

• Treatment by Baseline Score, p = 0.682

SE = Standard error; CI = Confidence interval.

a

Analyzed by ANCOVA model including effects for treatment, center, indication (DPN or PHN) and the

Baseline score value as covariate.

b

Adjusted P-value based on Hochberg’s procedure.



A supplemental analysis of endpoint mean scores for patients who did not complete the study

supported the results of the main analysis showing that pain reduction in both pregabalin

treatment groups was significantly greater than in placebo-treated patients.



Subgroup analyses performed by indication showed that in patients with PHN there were no

statistically significant differences in mean endpoint pain scores between the pregabalin flexible

and fixed dose groups compared with placebo (p= 0.115) but in patients with DPN both the

pregabalin flexible dose and fixed dose treatment groups were significantly different from the

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









placebo group (p= 0.009 and p = 0.006, respectively).



Responder analyses were performed in groups (patients with ≥30% and patients with a ≥50%

decrease in mean pain score from Baseline to endpoint). Results of the assessments in these 2

populations are given in Table S2.



Table S2 Results of Analysis of Responder Status: ITT Population

Treatment No. No. (%) of Treatment Comparisons

Assessed Responders (Placebo – Pregabalin)

Unadjusted P-Valuea Adjusted P-Valueb

Reduction ≥30%

Placebo 62 23 (37.1)

PGB Flexible Dose 139 82 (59.0) 0.003 0.003

PGB Fixed Dose 128 85 (66.4) <0.001 <0.001



Reduction ≥50%

Placebo 62 15 (24.2)

PGB Flexible Dose 139 67 (48.2) <0.001 <0.001

PGB Fixed Dose 128 67 (52.3) <0.001 <0.001

PGB= Pregabalin.

a

P-Value based on the results of the logistic regression with center, treatment, indication in the model, and Baseline

mean pain score as a covariate.

b

Adjusted P-value based on Hochberg’s procedure.



Repeated measures analysis was performed using all available weekly mean pain scores (post-

baseline) as the response. Overall, assessment of changes in mean pain scores from Baseline to

endpoint indicated that both pregabalin flexible and fixed dose treatment regimens were



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CLINICAL STUDY SYNOPSIS



significantly superior to placebo (both p <0.001). A pair-wise comparison of each pregabalin

dose versus placebo was performed at each time point. The pregabalin flexible dose treatment

group was statistically significantly different from placebo starting at Week 2 and continuing

through Week 12. The pregabalin fixed dose treatment group was statistically significantly

different from placebo starting at Week 1 and continuing through Week 12. This observation

may be related to the pregabalin dose level during the first week of treatment, which was

150 mg/day for the flexible dose group and 300 mg/day for the fixed dose group.



Secondary Efficacy Parameters

SF-MPQ Sensory, Affective, and Total Scores at Endpoint: Due to the heterogeneity of the SF-

MPQ across languages, these parameters could only be analyzed on English-speaking patients.

While patients in the pregabalin flexible and fixed dose treatment groups and patients who

received placebo experienced improvements from Baseline, no statistically significant

differences were observed for either treatment group compared with the placebo group in

improving SF-MPQ sensory scores, affective scores, and total scores at endpoint.



SF-MPQ Sensory, Affective, and Total Scores at Weeks 1, 2, 3, 4, 8 and 12: Statistically

significant differences from placebo were seen at Weeks 1 and 2 for the pregabalin flexible dose

(p= 0.050 and p= 0.023, respectively) and fixed dose (p= 0.015 and p= 0.004, respectively)

treatment groups for the Weekly SF-MPQ sensory score. While improvements in the SF-MPQ

sensory score were maintained throughout the remainder of the study, the differences from

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









placebo were not statistically significant for either pregabalin treatment group at Weeks 3, 4, 8,

or 12.



With the exception of the pregabalin fixed dose treatment group at Week 1 (p= 0.029), no

statistically significant differences from placebo were seen for the pregabalin flexible and fixed

dose treatment for English speaking subgroups for the Weekly SF-MPQ affective score.

Statistically significant differences from placebo were seen at Weeks 1 and 2 for the pregabalin

flexible dose (p= 0.026 and p= 0.013) and fixed dose (p= 0.005 and p= 0.008) treatment groups

for the Weekly SF-MPQ total score. While improvements in the SF-MPQ total score were

maintained throughout the remainder of the study, the differences from placebo were not

statistically significant for either pregabalin treatment group at Weeks 3, 4, 8, or 12.



Short-Form McGill Pain Questionnaire, Visual Analogue Scale, and PPI Scores at Endpoint:

Statistically significant differences were seen for both the pregabalin flexible and fixed dose

treatment groups when compared with placebo for endpoint VAS (both p <0.001). In addition,

statistically significant differences were seen for both the pregabalin flexible and fixed dose

treatment groups when compared with placebo for endpoint PPI (p= 0.014 and p= 0.012,

respectively).



Short-Form McGill Pain Questionnaire, Visual Analogue Scale, and PPI Scores at Weeks 1, 2,

3, 4, 8, and 12: Statistically significant differences were seen for both the pregabalin flexible

and fixed dose treatment groups when compared with placebo for VAS at Weeks 1, 2, 3, 4, and 8

(p ≤0.021). Statistically significant differences were seen for the pregabalin flexible dose

treatment group compared with placebo for PPI at Weeks 3 and 4 (p≤0.017) and for the

pregabalin fixed dose treatment group compared with placebo at Weeks 2, 3, and 4 (p≤0.017).



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CLINICAL STUDY SYNOPSIS



Endpoint Mean Sleep Interference Scores: A comparison of endpoint mean sleep interference

scores showed a statistically significant improvement for patients receiving either pregabalin

flexible or fixed dose compared with patients receiving placebo (p <0.001 for both comparisons).



Weekly Mean Sleep Interference Scores: In an ANCOVA analysis using all available weekly

mean sleep scores (post-baseline) as the response, pair-wise comparison of each pregabalin dose

versus placebo at each time point indicated that the weekly mean sleep interference scores for the

pregabalin flexible and fixed dose treatment group showed statistically significant decreases in

pain-related sleep interference for Weeks 1 to 5 (p ≤0.007 for both comparisons) and 9 to 12 (p

≤0.041 for both comparisons). Neither pregabalin dose group showed statistically significant

decreases compared with the placebo group for Weeks 6 to 8.



Medical Outcomes Study-Sleep Scale Scores: No significant difference from placebo was seen

for either pregabalin treatment group for the optimal sleep subscale. Assessment of percentages

of patients with and without optimal sleep at Baseline who did or did not achieve optimal sleep

at termination showed that 28.2% of 39 patients in the placebo treatment group who did not have

optimal sleep at Baseline achieved optimal sleep at termination. The respective values for 98

such patients in the pregabalin flexible dose treatment group and 97 patients in the pregabalin

fixed dose treatment group were 41.8% and 29.9%. Of the Medical Outcomes Study-Sleep

subscales scores, the pregabalin flexible and fixed dose treatment groups were statistically

significantly superior to the placebo group for sleep disturbance (p <0.001 and p <0.001,

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









respectively) and overall sleep problem index (p= 0.017 and p= 0.030, respectively).



Patient Global Impression of Change: The percentage of patients reporting improvement (rated

as very much, much, or minimal in global impression of change) was 74.4% for pregabalin

flexible dose and 71.2% for pregabalin fixed dose, compared with 47.5% for the placebo group.

Overall, there were statistically significant differences in the PGIC responses of both the

pregabalin flexible and fixed dose groups compared with the placebo treatment group (p ≤0.001).



Signs/Symptoms of Allodynia and Hyperalgesia: A summary of patients with signs and

symptoms of allodynia and hyperalgesia at baseline and endpoint by indication is presented in

Table S3.









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CLINICAL STUDY SYNOPSIS



Table S3 Summary of Allodynia and Hyperalgesia: Change From Baseline to Endpoint

(ITT Population)

Baseline Termination

Yes, N (%) No, N (%)

Patients with PHN

Allodynia

Placebo Yes (N = 8) 6 (75.0) 2 (25.0)

No (N = 7) 0 (0.0) 7 (100.0)

PGB Flexible Dose Yes (N = 22) 16 (72.7) 6 (27.3)

No (N = 10) 0 (0.0) 10 (100.0)

PGB Fixed Dose Yes (N = 23) 17 (73.9) 6 (26.1)

No (N = 8) 2 (25.0) 6 (75.0)

Hyperalgesia

Placebo Yes (N = 5) 3 (60.0) 2 (40.0)

No (N = 10) 3 (30.0) 7 (70.0)

PGB Flexible Dose Yes (N = 21) 14 (66.7) 7 (33.3)

No (N = 11) 2 (18.2) 9 (81.8)

PGB Fixed Dose Yes (N = 24) 18 (75.0) 6 (25.0)

No (N = 7) 1 (14.3) 6 (85.7)

Patients with DPN

Allodynia

Placebo Yes (N = 20) 15 (75.0) 5 (25.0)

No (N = 23) 0 (0.0) 23 (100.0)

PGB Flexible Dose Yes (N = 46) 33 (71.7) 13 (28.3)

No (N = 53) 2 (3.8) 51 (96.2)

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PGB Fixed Dose Yes (N = 49) 32 (65.3) 17 (34.7)

No (N = 43) 0 (0.0) 43 (100.0)

Hyperalgesia

Placebo Yes (N = 12) 9 (75.0) 3 (25.0)

No (N = 31) 2 (6.5) 29 (93.5)

PGB Flexible Dose Yes (N = 29) 13 (44.8) 16 (55.2)

No (N = 70) 1 (1.4) 69 (98.6)

PGB Fixed Dose Yes (N = 29) 20 (69.0) 9 (31.0)

No (N = 63) 1 (1.6) 62 (98.4)

PGB= Pregabalin.

Summary descriptive statistics are based on subjects with both Baseline and post-treatment data.



Short-Form 36 Health Survey: All 3 treatment groups showed improvements in all 8 of the SF-

36 domains. Although the pregabalin flexible dose gave greater improvements when compared

with placebo, only the results for the mental health domain showed statistical significance

(p= 0.001). The pregabalin fixed dose only showed numerical improvements over placebo for

the bodily pain, general health perception, social functioning and mental health domains; none of

these differences were statistically significant. In each domain the greatest improvements were

seen with the pregabalin flexible dose regimen.



EuroQOL Health Utilities Index —5 Domains Utility Score and Visual Analogue Scale: EQ-5D

utility and VAS area under the curve (AUC) scores for either pregabalin treatment group and

VAS scores for the pregabalin fixed dose treatment group were not statistically significantly

different when compared with placebo. However, VAS scores for the pregabalin flexible dose

treatment group but not the fixed dose treatment group were significantly improved from

Baseline to endpoint compared with placebo (p= 0.005).





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Safety Results: Of the 338 patients who received study medication, 224 (66.3%) experienced at

least 1 adverse event. The percentages of patients in the pregabalin flexible dose treatment group

who reported adverse events (97 patients, 68.8%) was slightly lower than that for the pregabalin

fixed dose treatment group (98 patients, 74.2%). The adverse event rate in each pregabalin

treatment group was higher than that for the placebo group (29 patients, 44.6%). A summary of

TESS adverse events occurring in at least 3.0% of patients in any pregabalin treatment group is

shown in Table S4.



Table S4 Summary of TESS Reported Adverse Eventsa by Decreasing Frequency: Safety

Population

Preferred Term N (%) of Patients

Placebo Pregabalin

N = 65 Flexible Dose Fixed Dose Any Dose

N = 141 N = 132 N = 273

Dizziness 3 (4.6) 29 (20.6) 38 (28.8) 67 (24.5)

Peripheral Edema 4 (6.2) 23 (16.3) 13 (9.8) 36 (13.2)

Weight Gain 2 (3.1) 18 (12.8) 18 (13.6) 36 (13.2)

Somnolence 0 (0.0) 15 (10.6) 17 (12.9) 32 (11.7)

Vertigo 1 (1.5) 11 (7.8) 14 (10.6) 25 (9.2)

Asthenia 1 (1.5) 10 (7.1) 14 (10.6) 24 (8.8)

Nausea 1 (1.5) 8 (5.7) 15 (11.4) 23 (8.4)

Accidental Injury 3 (4.6) 11 (7.8) 5 (3.8) 16 (5.9)

Headache 4 (6.2) 9 (6.4) 7 (5.3) 16 (5.9)

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









Diarrhea 0 (0.0) 11 (7.8) 4 (3.0) 15 (5.5)

Pain 2 (3.1) 8 (5.7) 5 (3.8) 13 (4.8)

Dry Mouth 3 (4.6) 4 (2.8) 8 (6.1) 12 (4.4)

Abnormal Vision 0 (0.0) 5 (3.5) 4 (3.0) 9 (3.3)

Hypertension 0 (0.0) 4 (2.8) 5 (3.8) 9 (3.3)

Constipation 4 (6.2) 4 (2.8) 4 (3.0) 8 (2.9)

Infection 2 (3.1) 5 (3.5) 3 (2.3) 8 (2.9)

Rash 1 (1.5) 3 (2.1) 5 (3.8) 8 (2.9)

Amnesia 0 (0.0) 3 (2.1) 4 (3.0) 7 (2.6)

Back Pain 2 (3.1) 5 (3.5) 2 (1.5) 7 (2.6)

Vomiting 3 (4.6) 2 (1.4) 5 (3.8) 7 (2.6)

Ataxia 1 (1.5) 0 (0.0) 5 (3.8) 5 (1.8)

Confusion 1 (1.5) 1 (0.7) 4 (3.0) 5 (1.8)

Dyspnea 0 (0.0) 5 (3.5) 0 (0.0) 5 (1.8)

Abdominal Pain 2 (3.1) 2 (1.4) 1 (0.8) 3 (1.1)

Pruritus 2 (3.1) 2 (1.4) 1 (0.8) 3 (1.1)

Cough Increased 2 (3.1) 0 (0.0) 0 (0.0) 0 (0.0)

a

Reported in at least 3% of patients in any of the treatment groups. Events are sorted by decreasing frequency in the

all pregabalin group.



Most adverse events were mild or moderate in intensity. Severe adverse events were reported by

23 (16.3%) patients in the pregabalin flexible dosing group, 25 (18.9%) patients in the pregabalin

fixed dosing group and 6 (9.2%) patients in the placebo group. Severe adverse events reported

by more than 2 patients were pain, dizziness and back pain in the pregabalin flexible dosing

group (reported by 4, 3 and 3 patients, respectively) and dizziness and somnolence in the

pregabalin fixed dosing group (6 and 4 patients, respectively).







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The percentage of patients who experienced associated adverse events was greatest among

patients in the pregabalin fixed dose treatment group (91 patients, 68.9%), lower among patients

in the pregabalin flexible dose treatment group (78 patients, 55.3%), and lowest in the placebo

group (18 patients, 27.7%). A summary of TESS associated adverse events occurring in at least

3.0% of patients in any pregabalin treatment group is shown in Table S5.



Table S5 Summary of TESS Reported Associated Adverse Eventsa by Decreasing

Frequency: Safety Population

Preferred Term N (%) of Patients

Placebo Pregabalin

N = 65 Flexible Dose Fixed Dose Any Dose

N = 141 N = 132 N = 273

Dizziness 3 (4.6) 27 (19.1) 38 (28.8) 65 (23.8)

Weight Gain 2 (3.1) 17 (12.1) 18 (13.6) 35 (12.8)

Peripheral Edema 2 (3.1) 22 (15.6) 10 (7.6) 32 (11.7)

Somnolence 0 (0.0) 15 (10.6) 17 (12.9) 32 (11.7)

Vertigo 1 (1.5) 11 (7.8) 13 (9.8) 24 (8.8)

Asthenia 0 (0.0) 9 (6.4) 12 (9.1) 21 (7.7)

Nausea 1 (1.5) 7 (5.0) 14 (10.6) 21 (7.7)

Dry Mouth 3 (4.6) 4 (2.8) 8 (6.1) 12 (4.4)

Headache 2 (3.1) 7 (5.0) 3 (2.3) 10 (3.7)

Abnormal Vision 0 (0.0) 4 (2.8) 4 (3.0) 8 (2.9)

Amnesia 0 (0.0) 2 (1.4) 4 (3.0) 6 (2.2)

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









Vomiting 2 (3.1) 1 (0.7) 5 (3.8) 6 (2.2)

Confusion 1 (1.5) 1 (0.7) 4 (3.0) 5 (1.8)

Constipation 2 (3.1) 2 (1.4) 3 (2.3) 5 (1.8)

Rash 0 (0.0) 1 (0.7) 4 (3.0) 5 (1.8)

Ataxia 1 (1.5) 0 (0.0) 4 (3.0) 4 (1.5)

Pruritus 2 (3.1) 1 (0.7) 1 (0.8) 2 (0.7)

a

Reported in at least 3% of patients in any of the treatment groups. Events are sorted by decreasing frequency in the

all pregabalin group.



There were 2 patient deaths reported during the study. One patient in the pregabalin fixed dose

group died due to cardiac arrest that was definitely not related to pregabalin. One patient in the

pregabalin flexible dose group died as a result of worsening chronic obstructive pulmonary

disease (COPD) that was considered to be unlikely to be related to pregabalin.



Seventeen patients experienced serious, nonfatal adverse events, including 2 placebo-treated

patients and 15 pregabalin-treated patients (10 in the pregabalin flexible dose treatment group

and 5 in the pregabalin fixed dose treatment group). A summary of all serious adverse events is

presented in Table S6.









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Table S6 Summary of Serious Adverse Eventsa by Decreasing Frequency

Preferred Term N (%) of Patients

Placebo Pregabalin

N = 65 Flexible Dose Fixed Dose Any Dose

N = 141 N = 132 N = 273

Angina Pectoris 0 (0.0) 2 (1.4) 0 (0.0) 2 (0.7)

Diabetes Mellitus 0 (0.0) 0 (0.0) 2 (1.5) 2 (0.7)

Angioedema 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Asthenia 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

BUN Increased 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Chest Pain 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Cholecystitis 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Coagulation Disorder 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Confusion 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Creatinine Increased 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Deep Thrombophlebitis 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Diabetic Acidosis 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Dizziness 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Dysarthria 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Heart Arrest 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Hyperglycemia 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Hypernatremia 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Hypovolemia 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Lung Disorder 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









Paralysis 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Petechial Rash 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Pneumonia 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Prostatic Specific Antigen 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Increase

Purpura 0 (0.0) 0 (0.0) 1 (0.8) 1 (0.4)

Varicose Vein 0 (0.0) 1 (0.7) 0 (0.0) 1 (0.4)

Vomiting 1 (1.5) 0 (0.0) 0 (0.0) 0 (0.0)

Weight Loss 1 (1.5) 0 (0.0) 0 (0.0) 0 (0.0)

BUN= Blood urea nitrogen.

a

Includes fatal and nonfatal serious AEs.



Sixty-two (62) patients withdrew from the study due to adverse events, including 5 (7.7%)

placebo-treated patients and 57 (20.9%) pregabalin-treated patients (24 [17.0%] in the pregabalin

flexible dose treatment group and 33 [25.0%] in the pregabalin fixed dose treatment group). Of

these, 45 (16.5%) pregabalin-treated patients withdrew due to adverse events that were

considered by investigators to be related to the study medication (17 [12.1%] patients in the

pregabalin flexible dose treatment group and 28 [21.2%] patients in the pregabalin fixed dose

treatment group). Among pregabalin-treated patients, adverse events that most frequently (in ≥5

patients) led to withdrawal were dizziness (13 [4.8%] patients), nausea (10 [3.6%] patients),

somnolence (5 [1.8%] patients), and vertigo (9 [3.3%] patients).



A review of median changes in clinically laboratory parameters generally indicated small

changes from Baseline that did not appear to differ significantly among treatment groups.

Patient vital signs, including weight, supine heart rate, and supine and standing systolic and

diastolic blood pressure, were examined for clinically important changes from Baseline to





Protocol 1008-155 / Page 10 of 11

PhrmaWebSynopsis-Final-15 September 2006

CLINICAL STUDY SYNOPSIS



termination using predefined criteria. Possibly clinically important changes in vital signs

included the following:



• A weight decrease (ratio to Baseline was ≤0.93) from Baseline to last visit: 2 patients (0

patients in the placebo group; 1 patient or 0.7% in the flexible dose pregabalin treatment

group and 1 patient or 0.8% in the pregabalin fixed dose treatment group)

• A weight increase (ratio to Baseline was ≥1.07) from Baseline to last visit: 28 patients (0

patients in the placebo group; 19 patients or 13.9% in the pregabalin flexible dose

treatment group; and 9 patients or 7.0% in the pregabalin fixed dose treatment group).



CONCLUSION(S):



In this 12-week study, twice-daily administration of pregabalin in the flexible dose (150-600

mg/day) or fixed dose (600 mg/day) regimens was statistically significantly superior to placebo

in relieving pain associated with either DPN or PHN. Pregabalin was shown to be safe and

generally well tolerated in both the flexible dose and fixed dose regimens. No new safety

concerns for pregabalin were identified in this study. Pregabalin 150-600 mg/day was shown to

be safe and generally well tolerated.

01000006061787 \ 1.1 \ Approved \ 20-Sep-2006 17:20









Protocol 1008-155 / Page 11 of 11

PhrmaWebSynopsis-Final-15 September 2006



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