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The safety and efficacy of this agent(s), or use in this setting, has not been established or is subject to confirmation. For an agent(s) whose safety and efficacy has not been established or confirmed, future regulatory approval or commercial availability is not guaranteed.
PF-07248144 is an investigational compound. Its safety and efficacy have not been established.
Active enrolling
United States, Australia, China, Japan, Korea, Republic of
EXPERIMENTAL: 1A Monotherapy Dose Escalation
PF-07248144 Monotherapy Escalation
DRUG: PF-07248144
KAT6 Inhibitor
EXPERIMENTAL: 1B Combination Dose Escalation
PF-07248144 with Fulvestrant Combination Dose Escalation
DRUG: PF-07248144
KAT6 Inhibitor
DRUG: Fulvestrant
Endocrine Therapy
EXPERIMENTAL: 1C Combination Dose Escalation
PF-07248144 with Letrozole + Palbociclib Combination Dose Escalation
DRUG: PF-07248144
KAT6 Inhibitor
DRUG: Letrozole
Endocrine Therapy
DRUG: Palbociclib
CDK4/6 Inhibitor
EXPERIMENTAL: 2A Monotherapy Dose Expansion Arm
PF-07248144 Monotherapy Dose Expansion
DRUG: PF-07248144
KAT6 Inhibitor
EXPERIMENTAL: 2B Combination Dose Expansion Arm
PF-07248144 with Fulvestrant Dose Expansion
DRUG: PF-07248144
KAT6 Inhibitor
DRUG: Fulvestrant
Endocrine Therapy
EXPERIMENTAL: 1D Combination Dose Escalation
PF-07248144 with PF-07220060 +Fulvestrant
DRUG: PF-07248144
KAT6 Inhibitor
DRUG: Fulvestrant
Endocrine Therapy
DRUG: PF-07220060
CDK4 inhibitor
EXPERIMENTAL: 2D Combination Dose Expansion Arm
PF-07248144 with PF-07220060 +Fulvestrant Dose Expansion
DRUG: PF-07248144
KAT6 Inhibitor
DRUG: Fulvestrant
Endocrine Therapy
DRUG: PF-07220060
CDK4 inhibitor
EXPERIMENTAL: China Monotherapy Dose Expansion
PF-07248144 Monotherapy Dose Expansion
DRUG: PF-07248144
KAT6 Inhibitor
Histological or cytological diagnosis of advanced or metastatic ER+HER2- breast cancer. Participants must have progressive disease after at least 1 prior line of a CDK4/6 inhibitor and at least 1 prior line of endocrine therapy.
Number of participants with dose-limiting toxicities in the Dose Escalation Arms.
Dose-limiting toxicities (DLTs)
Up to 29 days
Safety and Tolerability as assessed by adverse event monitoring for participants enrolled in the Dose Escalation Arms.
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Up to 24 months
Safety and Tolerability through monitoring of laboratory assessments for participants enrolled in the Dose Escalation Arms.
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
Up to 24 months
Safety and Tolerability as assessed by adverse event monitoring for participants enrolled in the Dose Expansion Arms
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Up to 24 months
Safety and Tolerability through monitoring of laboratory assessments for participants enroled in the Dose Expansion Arms
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
Up to 24 months
Single Dose: Maximum Observed Concentration (Cmax) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Single Dose: Time to Maximum concentration (Tmax) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Single Dose: AUC from time zero to time of last measurable concentration (AUClast) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Single and Multiple Dose: Terminal Elimination half-life (t1/2) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Multiple Dose: Steady-State Cmax (Cmax,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Multiple Dose: Steady-state Tmax (Tmax,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Multiple Dose: Steady state AUC during a dosage interval (τ) (AUCτ,ss) in the Dose Escalation and Dose Finding Arms
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Multiple Dose: Steady-state Cmin (Cmin,ss) in the Dose Escalation and Dose Finding Arms.
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Multiple Dose: Steady-state apparent total clearance (CLss/F) in the Dose Escalation and Dose Finding Arms.
Pharmacokinetic (PK) assessments for PF-07248144 and PF-07220060 (Part 1D)
Up to 24 months
Palbociclib trough concentrations at steady instate (Cmin,ss) in the 1C combination dose finding arm.
Pharmacokinetic (PK) assessment for palbociclib exposure.
Up to 24 months
Best Overall Response (BOR) in participants in the Dose Expansion Arms
Up to 24 months
Duration of Response (DOR) in participants enrolled in the Dose Expansion Arms
Up to 24 months
Peak concentrations of PF-07248144 and PF-07220060 (Part 2D) for selected cycles in the Dose Expansion Arms
Pharmacokinetic (PK) assessment for PF-07248144 and PF-07220060 (Part 2D)
Up to 24 months
Trough concentrations of PF-07248144 for selected cycles in the Dose Expansion Arms
Pharmacokinetic (PK) assessment for PF-07248144 and PF-07220060 (Part 2D)
Up to 24 months
Maximum Observed Concentration (Cmax) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF-07248144.
Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
Time to Maximum concentration (Tmax) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF-07248144.
Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
AUC from time zero to time of last measurable concentration (AUClast) in the participants in the food effect subset in monotherapy dose expansion arm
The effect of food on the PK of PF 07248144.
Cycle 1 Day -7 and Cycle 1 Day 1 (each cycle is 28 days)
Amount of PF-07248144 excreted in urine relative to dose administered (%) in a sub-set of participants in monotherapy dose expansion arm.
Evaluate urine pharmacokinetic (PK) of PF-07248144.
Up to 24 months
Renal clearance (CLr) in a sub-set of participants in monotherapy dose expansion arm
Evaluate urine pharmacokinetic (PK) of PF-07248144.
Up to 24 months
Progression Free Survival (PFS) observed in participants in the Dose Expansion Arms
Up to 24 months
Time to Progression (TTP) observed in participants enrolled in the Dose Expansion Arms
Up to 24 months
Overall survival (OS) observed in participants enrolled in Dose Expansion Arms
Up to 24 months
Best Overall Response (BOR) observed in participants in the dose expansion arms
Up to 24 months
Duration of Response (DOR) observed in participants in the dose expansion arms
up to 24 months
Clinical Benefit Rate (CBR) observed in participants in the Dose Expansion Arms
up to 24 months
186
Sponsor: Pfizer
Collaborator: None
For more information, call or email the Pfizer Clinical Trial Contact Center:
When calling, please reference this study number: