A Phase 1/2 Multi-Center, Randomized, Open-Label, Dose
Escalation Study to Determine the Maximum Tolerated
Dose, Safety, and Efficacy of Pomalidomide Alone or in
Combination With Low-Dose Dexamethasone in Patients
With Relapsed and Refractory Multiple Myeloma (MM)
Who Have Received Prior Treatment That Includes
Lenalidomide and Bortezomib
Paul Richardson1, David Siegel2, Rachid Baz3, Susan L Kelley4,
Nikhil C Munshi
1, Daniel Sullivan3, Melissa Alsina3, Deborah Doss1,
Laura McBride
2, Gail Larkins5, Maria Lizza5, Min Chen5, Mohamed Zaki5,
Christian Jacques
5, Kenneth C Anderson1
1
Dana-Farber Cancer Institute, Boston, MA; 2Hackensack University
Medical Center, Hackensack, NJ;
3H. Lee Moffitt Cancer Center and
Research Institute, Tampa, FL;
4Multiple Myeloma Research Consortium,
Norwalk, CT;
5Celgene Corporation, Summit, NJ
1
Disclosures
·
Membership of Advisory Committees:
­ Celgene Corporation
­ Millennium
­ Johnson & Johnson
·
Research Support / PI:
­ Celgene Corporation
­ Millennium
2
1

Introduction
·
Pomalidomide (POM) is a distinct immunomodulatory agent that
has demonstrated direct anti-myeloma effects in lenalidomide-
refractory patients (pts) with significant antiproliferative activity
in vitro
1-2
·
POM has promising activity in relapsed multiple myeloma (MM)
across a dose range of 2 ­ 5 mg dosed continuously
3
·
POM at 4 mg for 21 of 28 days as monotherapy and in
combination with low-dose dexamethasone (dex) is active and
well tolerated in pts with relapsed and refractory MM
4
O
O
H N
O
N
Pomalidomide
O
NH
2
1. Hideshima et al. Blood. 2000;96(9):2943-50. 2. Mitsiades et al. Blood. 2002;99:4525-30.
3. Schey et al. J Clin Oncol 22:3269-76. 4. Richardson et al. Blood. 2010;116:377-8 [abstract 864].
3
Introduction (cont.)
·
POM has clinical efficacy in relapsed MM pts following LEN
treatment at a dose of 2 mg given continuously with low-dose dex
Phase 2 Study: POM 2 mg + low-dose dex
1-3
ORR
PFS
OS
1-3 prior therapies
1
63%
11.6 mos
94% at 6 mos
Refractory to LEN
2
32%
4.8 mos
13.9 mos
Refractory to LEN & Bz
3
26%
8 mos
86% at 6 mos
·
MM002 (Phase 1) evaluated POM 21 of 28 days ± low-dose dex to
explore higher doses ranging from 2 to 5 mg
4
­ Relapsed and refractory MM
­ Received both LEN & bortezomib (Bz): refractory to last therapy
·
MM002: Phase 1 (as of June 2010) and preliminary Phase 2 data
(as of October 2010) are presented
1. Lacy et al. J Clin Oncol. 2009;27:5008-14. 2. Lacy et al. Leukemia. 2010;24(11):1934-9. 3. Lacy et al. ASCO 2010
Presentation [Abstract 8002]. 4. Richardson et al. Blood. 2009;114:126-7 [abstract 301].
4
2

MM-002 Study Schema
POM ± low-dose dex in Relapsed and Refractory MM
Phase 1 (MTD)
Dose
Discontinue
2 mg
POM therapy
Progressive disease (PD)
Option to add
and follow-up
PD
(QD on days 1-21 of
for survival
3 mg
dex
or no response after
and
a 28 day cycle)
(40 mg/wk)
4 mg
completion of 4 cycles
subsequent
treatment
5 mg
Phase 2 (Open Label)
PD
Discontinue
ON
Arm A
and follow-up
TI
POM (4 mg) + dex
A
for survival
Z
and
subsequent
treatment
PD
Option to add
NDOMI
Arm B
low-dose dex
RA
POM (4 mg)
(40 mg/wk)
Concomitant Medications: anti-coagulants, G-CSF use after Cycle 1, erythroid growth
factors, bisphosphonates, transfusions with platelet, RBCs as clinically indicated .
5
MM-002 Study Design
POM ± low-dose dex in Relapsed and Refractory MM
·
Selected key inclusion criteria:
­ 18 yrs of age
­ Relapsed and refractory MM
1
Measurable levels of M paraprotein in serum or urine
2 prior therapies: progressing on treatment or within
60 days of last therapy
Prior treatment with 2 cycles of LEN and 2 cycles of
Bz (either in separate regimens or within the same
regimen)
·
Primary endpoints:
­ Phase 1: MTD
­ Phase 2: PFS
·
Secondary endpoints: response (modified EBMT and IMWG
criteria)
2-4, time to response, duration of response (DOR), OS,
safety
1. Anderson et al. Leukemia. 2008;22(2):231-9. 2. Blade et al. Br J Haematol. 1998;102(5):1115-23. 3. Richardson et al.
N Engl J Med. 2003;348(26):2609-17. 4. Durie et al. Leukemia. 2006;20(9):1467-73.
6
3

MM-002: Phase 1
MTD, Efficacy, Safety, and Statistical Analysis
· MTD - the highest dose at which >2 of 6 pts
experienced a DLT within the first 28-day cycle
­ MTD determined using a "3 + 3" design
­ Safety analyses: DLTs summarized at conclusion of
each dose level
· Efficacy assessments carried out every 28 days
following completion of the first cycle
· DMC review of efficacy and safety data completed
­ Safety assessed using NCI CTC for AE v 3.0
DLT: Dose-limiting toxicity; MTD: Maximum tolerated dose; DMC: Data Monitoring Committee; NCI CTC: National
Cancer Institute Common Toxicity Criteria; AE: Adverse event
7
MM-002: Phase 1
Demographics
2 mg
3 mg
4 mg
5 mg
Total
(n = 6)
(n = 8)
(n = 14)
(n = 10)
(N = 38)
66
72
69
64
67
Median age (range), yrs
(55-72)
(61-78)
(45-80)
(38-83)
(38-83)
Male, %
17
38
71
40
47
Caucasian, %
83
100
100
80
92
Median # prior therapies
8
6
6
6
6
(range)
(5-14)
(2-12)
(2-17)
(3-10)
(2-17)
Prior LEN and Bz, %
100
100
100
100
100
Prior dexamethasone, %
100
100
100
100
100
Prior thalidomide, %
67
75
79
90
79
Prior SCT, %
67
75
79
60
66
·
84% aged 75 yrs
·
82% ISS stage II/III disease
·
28% pts received prior carfilzomib
8
4

MM-002: Phase 1
Disposition
2 mg
3 mg
4 mg
5 mg
Total
(n = 6)
(n = 8)
(n = 14) (n = 10) (N = 38)
n
n
n
n
n
Discontinuation
6
8
12
7
33
PD
2
353
13
AE
a
1
021
4
Withdrew consent
1
1
2
2
6
Death
b
0
120
3
·
Rate of discontinuation due to AE was low (11%)
·
No treatment-related mortality
a. Includes thrombocytopenia, anemia, gastrointestinal hemorrhage, vomiting, chills, fatigue, pyrexia, metastases
to meninges, renal failure, and rash.
b. Not related to study drug (pneumonia due to infection; gastrointestinal hemorrhage; bacterial meningitis and
subarachnoid hemorrhage).
9
MM-002: Phase 1
Adverse Events
2 mg
3 mg
4 mg
5 mg
Total
(n = 6)
(n = 8)
(n = 14)
(n = 10) (N = 38)
n
n
n
n
n
G3/4 AE
Neutropenia
1
4
7
8
20
Anemia
4
220
8
Thrombocytopenia
1
2
1
2
6
Fatigue
2
1
3
1
7
Peripheral neuropathy
1
0
1
3
5
VTE
2
011
4
SAE and dose reductions
SAEs
3
4
8
4
19
POM dose reduction
0
1
3
10
14
·
Manageable toxicity
­
Most common AEs (all grades): neutropenia (47%), fatigue (32%), anemia (24%), and
muscle spasms (18%)
SAEs, severe adverse events; VTE, venous thromboembolism
10
5

MM-002: Phase 1
Dose-Limiting Toxicities
Completed Cycles,
a
DLTs
POM Dose
Median (range)
(Reason)
2 mg (n = 6)
1.5 (1-12)
1 (G3 fatigue)
3 mg (n = 8)
5.0 (2-12)
1 (G4 neutropenia)
4 mg (n = 14)
5.5 (1-20)
2 (G4 neutropenia)
5 mg (n = 10)
8.0 (1-16)
4 (G4 neutropenia)
·
Pts received a median of 5 (range 1-20) cycles of POM
·
All but 1 of the DLTs due to G4 neutropenia
·
MTD determined to be 4 mg
a. During the dose-escalation phase, G-CSF was not allowed during Cycle 1 (ie, initial 28 days).
11
MM-002: Phase 1
Best Response & Clinical Outcome: POM ± low-dose dex
(Evaluable Pts
a)
80
PR: 29%
CR
PR
MR
MR: 71%
b
70
PR: 27%
60
MR: 55%
b
PR: 25%
MR: 50%
)
50
43%
(%
PR: 33%
ts
40
27%
MR: 33%
PR: 14%
25%
MR: 29%
b
leP
30
abu
20
14%
al
33%
v
27%
29%
21%
E
10
14%
4%
0
2 mg (n = 3)
3 mg (n = 7)
4 mg (n = 11)
5 mg (n = 7)
Total (N = 28)
DOR
c, median wks
20
24
16
Not reached
20
PFS, median wks
31
36
12
20
20
OS, median wks
81
80
Not reached
Not reached
80
·
Pts who received POM 4 or 5 mg achieved higher response rates
compared to those who received 2 or 3 mg
a. Includes eligible, treated and evaluable for efficacy assessment; b. Discrepancies in totals due to rounding
c. Assessed for responders only: 2mg (1); 3mg (1); 4mg (3); 5mg (2); total (7)
12
6

MM-002: Phase 2
Status and Update
·
Study ongoing: Phase 2 enrollment completed
in September 2010 (N=221)
·
Data analysis performed on first 120 efficacy
evaluable pts (enrolled by April 30, 2010)
·
Central Adjudication Committee review of
Phase 2 response data in process
·
Aggregate data on response results based on
investigator assessment (Oct 29, 2010 cut-off)
13
MM-002: Phase 2 Preliminary Results
Demographics
Total
Relapsed and Refractory Myeloma
N=120
Median age, yrs (range)
63 (34 - 88)
75, %
89
>75, %
11
Male, %
55
Caucasian, %
79
Median time since diagnosis, yrs (range)
6 (1 - 18)
Median # prior therapies (range)
5 (2 - 13)
Prior LEN & Bz, %
100
Prior thalidomide, %
74
Prior SCT, %
79
Double refractory to both prior LEN & Bz, n (%)
38 (32)
ECOG performance status score, %
023
164
210
Pending
3
14
7

MM-002: Phase 2 Preliminary Results
Efficacy (Aggregate Data)
Best Response in Efficacy Evaluable Pts
(Modified EBMT Criteria)
N = 120
n (%)
PR
30 (25)
CR
1 (1)
PR
29 (24)
MR
16 (13)
SD
64 (53)
PD
10 (8)
CR: complete response; PR: partial response; MR: minimal response; SD: stable disease;
PD: progressive disease
15
MM-002: Phase 2 Preliminary Results
Efficacy (Aggregate Data)
Best Response According to Refractoriness to Prior Therapy*
(Modified EBMT Criteria)
Refractory to
Refractory to
Double Refractory
LEN
Bz
(LEN & Bz)
N = 64
N = 51
N = 38
n (%)
PR
15 (23)
13 (26)
11 (29)
MR
21 (33)
19 (37)
13 (34)
CR
0
1 (2)
0
PR
15 (23)
12 (24)
11 (29)
MR
6 (9)
6 (11)
2 (5)
SD
36 (56)
25 (49)
20 (53)
PD
7 (10)
7 (14)
5 (13)
* Among the 120 efficacy evaluable pts, 64 were refractory to LEN, 51 refractory to
Bz, 38 were refractory to both LEN and Bz
16
8

MM-002: Phase 2 Preliminary Results
Efficacy with or without Cytogenetic
Abnormalities (Aggregate Data)
Best Response
(Modified EBMT Criteria)
With
Without
Cytogenetic Abnormalities*
Cytogenetic Abnormalities
N = 45
N = 74
n (%)
n (%)
PR
8 (18)
22 (30)
CR
0 (0)
1 (1)
PR
8 (18)
21 (28)
MR
8 (18)
8 (11)
SD
25 (56)
38 (51)
PD
4 (9)
6 (8)
*Presence of at least one of the following at baseline: del13q14, del17p13, t(4p13;14q32), t(14q32;16q23)
17
MM-002: Phase 2 Preliminary Results
Safety (Aggregate Data)
Total
G3/4 Events
N = 120
of Clinical Importance
%
Hematologic
Neutropenia
42
Thrombocytopenia
22
Anemia
20
Febrile neutropenia
5
Non-Hematologic
Infections
31
Fatigue
12
Renal failure
7
Cardiac disorders
a
4
DVT
1
Peripheral neuropathy
0
a. Cardiac disorders include: atrial fibrillation, myocardial ischemia, CHF
18
9

MM-002: Conclusions
POM ± low-dose dex in Relapsed and Refractory MM
·
Manageable toxicity profile in heavily pretreated pts status-post
LEN & Bz
­ MTD: 4 mg days 1-21 of a 28-day cycle
­ Most common hematologic G3/4 AE: myelosuppression
·
Very low incidence of G3/4 PN and DVT
·
Clinically meaningful responses in relapsed and refractory pts
status-post LEN & Bz
­ Median lines of prior therapy:
6 in Phase 1
5 in Phase 2
­ Phase 1 (evaluable pts):
PR: 25%; MR: 50%
Median DOR: 20 wks
Median PFS: 20 wks
Median OS: 80 wks
19
MM-002: Conclusions
POM ± low-dose dex in
Relapsed and Refractory MM
·
Phase 2 (aggregate data):
­ PR 25%; MR 38%
­ Median DOR: not reached
·
Double refractory to both LEN & Bz
­ PR 29%; MR 34%
­ Median DOR: not reached
·
POM has activity in pts who have cytogenetic
abnormalities
20
10

Future Directions
·
Final analysis of Phase 2 (N=221)
·
Analysis of gene expression profiling/surrogates
·
Additional study in relapsed and refractory MM now
enrolling
·
Future studies to use 4 mg on days 1-21 of each 28-day
cycle
·
Further dose exploration in less heavily pre-treated pts
·
Novel combinations (e.g. POM/Bz/dex, second-
generation proteasome inhibitors, alkylating agents,
clarithromycin/dex, other small molecules, MoABs)
21
Acknowledgements
Phase 2 Investigators Including:
Ravi Vij, Craig Hofmeister, Sundar Jagannath, Christine Chen
Sagar Lonial, Andrzej Jakubowiak, Nizar Bahlis, Kevin Song
Andrew Belch, Noopur Raje
Institutions with Study Sites
The Cancer Center - Hackensack University
St. Vincent's Comprehensive Cancer Center
Medical Center
University of Pittsburgh Cancer Institute
H. Lee Moffitt Cancer and Research Institute
Emory University
Massachusetts General Hospital
Princess Margaret Hospital - UHN
Mayo Clinic Arizona
Cross Cancer Center
Mayo Clinic Minnesota
University of Calgary - Tom Baker Cancer Center
Roswell Park Cancer Institute
Vancouver General Hospital, Diamond Health
The Ohio State University - James Cancer
Care Centre
Hospital
Royal Victoria Hospital - McGill University
University of Michigan Comprehensive Cancer
Multiple Myeloma Research Consortium
Center
Clinical Research Staff
Washington University - Siteman Cancer Center
Celgene Corporation
Our Patients and Families
22
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