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PF-05212384

Phase 1

Healthy | Small molecule | Other |Pfizer, Inc.|Last Updated: Sep 13, 2022

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment6

FDA Designations

No designations recorded

Clinical trial landscape

PF-05212384 · 3 trials · 3 indications

Phase 1 3
NCT02142920Investigation Of The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male VolunteersHealthy
COMPLETED6 Analytics
NCT01920061A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin in Patients With Triple Negative Breast Cancer in an Expansion Arm (TNBC)Neoplasm
COMPLETED110 Analytics
NCT00940498Study of PF-05212384 (Also Known as PKI-587)Administered Intravenously To Subjects With Solid TumorsNeoplasms
COMPLETED78 Analytics
PHASE1COMPLETED
Investigation Of The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male Volunteers
HealthyUnlock trial analytics
PHASE1COMPLETED
A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin in Patients With Triple Negative Breast Cancer in an Expansion Arm (TNBC)
NeoplasmUnlock trial analytics
PHASE1COMPLETED
Study of PF-05212384 (Also Known as PKI-587)Administered Intravenously To Subjects With Solid Tumors
NeoplasmsUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Observed Plasma Concentration (Cmax)
0.5 hours
Time to Reach Maximum Observed Plasma Concentration (Tmax)
0.5 hours
Number of Participants With Dose Limiting Toxicities (DLTs) - Arms A, B and C
Up to 21 days

DLT was defined as any of the following adverse events (AEs) attributable to the combination: (1) hematologic: grade 4 neutropenia lasting \>7 days; febrile neutropenia; grade \>=3 neutropenia with infection; grade 3 thrombocytopenia with bleeding; grade 4 thrombocytopenia; (2) non-hematologic: grade \>=2 pneumonitis; grade\>=3 toxicities, except pneumonitis, and excluding those that had not been maximally treated; persistent, intolerable toxicities which resulted in the failure to deliver at least 3 of the 4 doses of PF-05212384 for Arms A and B or at least 3 of the 4 doses of PF-05212384 and 75% of dacomitinib for Arm C during the first cycle; the persistent, intolerable toxicities which result in delay of the start of the second cycle by more than 2 weeks relative to the scheduled start; in an asymptomatic participant, the grade 3 QTc prolongation persists after correction of any reversible causes.

Percentage of Participants With Objective Response - Arm B Expansion
Cycle 1 Day 1 up to 18 months

Percentage of participants with objective response based on the assessment of confirmed complete response (CR) or confirmed partial response (PR) according to Response Evaluation Criteria in Solid Tumors (RECIST v1.1). Confirmed responses are those that persist on repeat imaging study at least 4 weeks after initial documentation of response. Per RECIST v1.1: CR was defined as complete disappearance of all target lesions and non-target disease, with the exception of nodal disease. All nodes, both target and non-target, must decrease to normal (short axis \<10 mm) and no new lesions. PR was defined as \>=30% decrease under baseline of the sum of diameters of all target lesions. The short axis was used in the sum for target nodes, while the longest diameter was used in the sum for all other target lesions. No unequivocal progression of non-target disease and no new lesions.

Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
Baseline up to Cycle 14 (each cycle is 28 days)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent were events between first dose of study drug and up to Cycle 14, that were absent before treatment or that worsened relative to pre-treatment state. AEs included both serious and non-serious adverse events.

Number of Participants With Treatment-Emergent Treatment-Related Adverse Events (AEs) or Serious Adverse Events (SAEs)
Baseline up to Cycle 14 (each cycle is 28 days)

Treatment-related AE was any untoward medical occurrence attributed to study drug in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to Cycle 14, that were absent before treatment or that worsened relative to pretreatment state. Relatedness to drug was assessed by the investigator. Participants with multiple occurrences of an AE within a category were counted once within the category. AEs included both serious and non-serious adverse events.

Number of Participants With Laboratory Abnormalities
Baseline up to Cycle 14 (each cycle is 28 days)

Criteria for laboratory test abnormality: hematology (hemoglobin \[less than {\<} 0.8\*lower limit of normal {LLN}\], platelets \[\<0.5\*LLN or greater than {\>} 1.75\*upper limit of normal {ULN}\], white blood cells \[\<0.6\*LLN or \>1.5\*ULN\], lymphocytes \[\<0.8\*LLN or \>1.2\*ULN\], total neutrophils \[\<0.8\*LLN or \>1.2\*ULN\], basophils, eosinophils, monocytes \[\>1.2\*ULN\]); coagulation \[partial thromboplastin time, prothrombin (PT), PT international ratio \[\>1.1\*ULN\]); liver function (total bilirubin \[\>1.5\*ULN\], aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase, alkaline phosphatase \[\>0.3\*ULN\], total protein, albumin \[\<0.8\*LLN or \>1.2\*ULN\]).

Number of Participants With Dose Limiting Toxicities (DLTs)
Baseline up to Day 28

DLT was defined as any of the following events occurring during the first 28 days of study medication and considered at least possibly-related to study medication: Grade 3 nonhematologic AE (including nausea, vomiting, or diarrhea despite optimal therapy; or greater than or equal to \[\>=\] grade 3 asthenia \>2 days; or fasting serum glucose \>250 milligrams per deciliter (mg/dL) despite optimal therapy); \>=Grade 4 thrombocytopenia; Grade 3 thrombocytopenia with bleeding; Grade 4 neutropenia lasting more than 7 days; Febrile neutropenia; other Grade 4 hematologic AE; delay of treatment \>2 consecutive weeks due to toxicity. Grades were based on National Cancer Institute Common Terminology Criteria for Adverse Events version 4.0.

Recommended Phase-2 Dose (RP2D)
Baseline up to Cycle 14 (each cycle is 28 days)

RP2D of PF-05212384 was determined based on the safety profile including laboratory and clinical assessments and pharmacodynamics findings.

Secondary Endpoints

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
9 Days
Area under the Concentration-Time Curve (AUC)
9 days
Plasma Decay Half-Life (t1/2)
9 days
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
[14C] PF 05212384EXPERIMENTALReceive PF-05212384 89 mg Dose
Arm AEXPERIMENTAL -
Arm BEXPERIMENTAL -
Arm CEXPERIMENTAL -
Expansion Arm 1EXPERIMENTAL -
Expansion Arm 2EXPERIMENTAL -
1EXPERIMENTALPF-05212384 (also known as PKI-587)

Interventions

NameTypeDescription
PF-05212384DRUGSingle 89 mg Dose via 30 minute IV infusion
PF-05212384 (gedatolisib)DRUGPF-05212384 weekly intravenous infusions starting at 90 mg/wk as a 3 week cycle
DocetaxelDRUGDocetaxel intravenous infusions once every 3 weeks starting at 75 mg/m\^2
CisplatinDRUGCisplatin intravenous infusions once every 3 weeks starting at 75 mg/m\^2
DacomitinibDRUGDacomitinib to be taken orally as a continuous once daily regimen at a starting dose of 30 mg
PF-05212384 (also known as PKI-587)DRUGIntravenous dosing once weekly infusion
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Eligibility Criteria

Age Range30 Years to 65 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy male subjects between the ages of 30- 65 years vasectomised or \>40 with no desire to father children in the near future (12 months), inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examinati...

Countries:United KingdomUnited StatesCanadaItalySpain
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Frequently asked questions about PF-05212384

What is PF-05212384 used for?

PF-05212384 is an investigational small molecule being studied for the treatment of neoplasms, including solid tumors and triple negative breast cancer. It has also been evaluated in healthy volunteers for metabolism and excretion studies. The drug is in Phase 1 clinical development and is not yet approved.

Who makes PF-05212384?

PF-05212384 is being developed by Pfizer, Inc., a biopharmaceutical company listed on the New York Stock Exchange under the ticker symbol PFE. The drug is currently in Phase 1 clinical trials, and Pfizer is conducting studies to evaluate its safety and efficacy in patients with various cancers.

What phase is PF-05212384 in?

PF-05212384 is in Phase 1 clinical development. All three clinical trials for the drug have been completed, and there are no active trials currently enrolling. The drug is investigational and has not received regulatory approval for any indication.

What clinical trials is PF-05212384 in?

PF-05212384 has been studied in three completed Phase 1 trials. NCT00940498 evaluated the drug intravenously in patients with solid tumors. NCT01920061 tested it in combination with other anti-tumor agents and cisplatin in triple negative breast cancer. NCT02142920 investigated its metabolism and excretion in healthy male volunteers.

Is PF-05212384 the same as PKI-587?

Yes, PF-05212384 is also known as PKI-587. In clinical trial NCT00940498, the study title refers to the drug as PF-05212384 (Also Known as PKI-587). This alternative name may appear in scientific literature and other references to the drug.