Phase 1
N=99
Study Of PF-00562271, Including Patients With Pancreatic, Head And Neck, Prostatic Neoplasms
Head and Neck Neoplasm · Prostatic Neoplasm · Pancreatic Neoplasm
Bottom Line
View on ClinicalTrials.gov: NCT00666926 ↗Enrolled (actual)
99
Serious AEs
27.3%
Results posted
Jun 2012
Primary outcome: Primary: Number of Participants With First Cycle Dose Limiting Toxicities (DLTs) — 0; 0; 0; 0 participants
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- PF00562271 (Drug)
- Age
- Adult, Older Adult · 18+ yrs
- Sex
- All
- Sponsor
- Verastem, Inc.
- Primary completion
- Apr 2009
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Number of Participants With First Cycle Dose Limiting Toxicities (DLTs) |
0; 0; 0; 0; 0; 0 | — |
| PRIMARY Percentage of Participants With Tumor Metabolic Response (Reduction of ≥15%) in Positron Emission Tomography With F-18-fluorodeoxyglucose (FDG-PET) |
50 | — |
| SECONDARY Maximum Serum Concentration (Cmax): PF-00562271 C0.D1, C1.D1 |
49.63; 71.13; 138.8; 130.1; 306.1; 312.9 | — |
| SECONDARY Maximum Serum Concentration (Cmax): PF-00562271 C1.D14 |
74.65; 134.7; 309.6; 307.7; 655.4; 1105 | — |
| SECONDARY Time to Reach Maximum Observed Serum Concentration (Tmax): PF-00562271 C0.D1, C1.D1 |
0.500; 1.50; 0.500; 0.500; 1.00; 1.50 | — |
| SECONDARY Time to Reach Maximum Observed Serum Concentration (Tmax): PF-00562271 C1.D14 |
0.500; 1.00; 1.00; 1.50; 2.00; 1.00 | — |
| SECONDARY Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast): PF-00562271 C0.D1, C1.D1 |
81.13; 233.8; 348.1; 295.6; 1205; 2364 | — |
| SECONDARY Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf): PF-00562271 C0.D1, C1.D1 |
86.24; 239.6; 354.1; 574.1; 1222; 2399 | — |
| SECONDARY Serum Decay Half-life (t 1/2): PF-00562271 C0.D1, C1.D1 |
1.990; 2.078; 2.173; 2.837; 2.897; 5.270 | — |
| SECONDARY Apparent Oral Clearance (CL/F): PF-00562271 C0. D1, C1.D1 |
964.2; 702.1; 707.2; 726.0; 478.0; 312.3 | — |
| SECONDARY Minimum Observed Serum Trough Concentration (Cmin): PF-00562271 C1.D14 |
0.01349; 0.8059; 48.96; 33.11; 145.8; 315.3 | — |
| SECONDARY Area Under the Curve From Time Zero to the End of the Dosing Interval (AUCtau): PF-00562271 C1.D14 |
156.3; 447.2; 1573; 1476; 4519; 8357 | — |
| SECONDARY Observed Accumulation Ratio (Rac): PF-00562271 C1.D14 |
1.864; 2.997; 4.522; 5.061; 3.899; 5.038 | — |
| SECONDARY Maximum Serum Concentration (Cmax): MDZ |
13.14; 20.40 | — |
| SECONDARY Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast): MDZ |
42.44; 134.0 | — |
| SECONDARY Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf): MDZ |
49.79; 212.3 | — |
| SECONDARY Time to Reach Maximum Observed Serum Concentration (Tmax): MDZ |
0.500; 1.00 | — |
| SECONDARY Serum Decay Half-life (t 1/2): MDZ |
5.045; 7.764 | — |
| SECONDARY Apparent Oral Clearance (CL/F): MDZ |
20090; 4709 | — |
| SECONDARY Percentage of Participants With Best Overall Response as Measured Using the Response Evaluation Criteria in Solid Tumors (RECIST) |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Phosphorylated Focal Adhesion Kinase (pFAK) |
— | — |
| SECONDARY Phosphorylated Mitogen Activated Pathway Kinase (pMAPK) |
— | — |
| SECONDARY Phospho-SRC (pSRC) |
— | — |
| SECONDARY Caspase-3 |
— | — |
Summary
Phase 1 safety, pharmacokinetics, and pharmacodynamics trial of the focal adhesion kinase (FAK) inhibitor PF-00562271 in patients with positive Positron Emission Tomography [PET] scans due to advanced non-hematologic malignancies, including pancreatic, head and neck, and prostatic neoplasms, and patients with other malignancies appropriate for serial biopsy. Screening consists of a Fluorodeoxyglucose Positron Emission Tomography [FDG-PET] and tumor imaging, medical history, physical examination, Eastern Cooperative Oncology Group [ECOG] performance status, blood draws, a pregnancy test for female patients of childbearing potential. Treatment consists of PF00562271 tablets continued until progression of disease, unacceptable toxicity, or patient request. Evaluations for bioactivity are measured by serial FDG-PET and blood tests for biomarkers related to FAK and PYK2 kinase activities.
Eligibility Criteria
Inclusion Criteria
- Pancreatic, head and neck, and prostatic neoplasms, and patients with non-hematologic malignancies who have tumor appropriate for serial biopsy.
- Adequate organ function, including bilirubin less than 1.5 x ULN, and [Eastern Cooperative Oncology Group] ECOG performance status of 0-2.
Exclusion Criteria
- Clinically significant gastrointestinal abnormalities, requirement for systemic anticoagulants or potent CYP 3A4 inhibitors, and history of clinically significant cardiac or pulmonary disorders.
Data sourced from ClinicalTrials.gov (NCT00666926). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.