Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
PF-07248144 · 7 trials · 6 indications
Dose-limiting toxicities (DLTs)
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
Adverse Events as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), timing, seriousness, and relationship to study therapy.
Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version 5.0), and timing.
AUClast will be used as the primary endpoint if AUCinf cannot be reliably estimated
To characterize the extent of excretion of total radioactivity in urine, feces, and vomitus (if any) following administration of a single oral dose of \[14C\]PF-07248144.
To characterize the metabolic profile and identify circulating and excreted metabolites following administration of a single oral dose of \[14C\]PF-07248144.
| Arm | Type | Description |
|---|---|---|
| Arm A: PF-07248144 plus fulvestrant | OTHER | PF-07248144 tablet taken by mouth plus fulvestrant taken as a shot into the muscle. |
| Arm B: everolimus plus ET | ACTIVE_COMPARATOR | Everolimus tablet taken by mouth plus investigator's choice of endocrine therapy of exemestane tablet taken by mouth or fulvestrant taken as a shot into the muscle. |
| 1A Monotherapy Dose Escalation | EXPERIMENTAL | PF-07248144 Monotherapy Escalation |
| 1B Combination Dose Escalation | EXPERIMENTAL | PF-07248144 with Fulvestrant Combination Dose Escalation |
| 1C Combination Dose Escalation | EXPERIMENTAL | PF-07248144 with Letrozole + Palbociclib Combination Dose Escalation |
| 2A Monotherapy Dose Expansion Arm | EXPERIMENTAL | PF-07248144 Monotherapy Dose Expansion |
| 2B Combination Dose Expansion Arm | EXPERIMENTAL | PF-07248144 with Fulvestrant Dose Expansion |
| 1D Combination Dose Escalation | EXPERIMENTAL | PF-07248144 with PF-07220060 +Fulvestrant |
| 2D Combination Dose Expansion Arm | EXPERIMENTAL | PF-07248144 with PF-07220060 +Fulvestrant Dose Expansion |
| China Monotherapy Dose Expansion | EXPERIMENTAL | PF-07248144 Monotherapy Dose Expansion |
| 1E Combination Dose Escalation | EXPERIMENTAL | PF-07248144 with Vepdegestrant Combination Dose Escalation |
| 2E Combination Dose Expansion Arm | EXPERIMENTAL | PF-07248144 with Vepdegestrant Combination Dose Expansion |
| PF-07248144 with and without Itraconazole | EXPERIMENTAL | Period 1; PF-07248144 single dose, oral tablet on Day 1. Period 2; Itraconazole oral solution once daily on Days 1-12 plus PF-07248144 single dose, oral tablet on Day 4. Period 1 and Period 2 will be separated with a washout of at least 14 days |
| Cohort 1 | EXPERIMENTAL | Participants will receive one dose of \[14C\] PF-07248144 by mouth in Period 1. After a washout, participants will receive one dose of PF-07248144 by mouth and one intravenous (IV) infusion of \[14C\] PF-07248144 in Period 2 |
| PF-07248144 with and without Carbamazepine | EXPERIMENTAL | PF-07248144 administered as a single dose in Period 1 on Day 1 and in Period 2 on Day 14. Carbamazepine administered once a day for Day 1 through 3, then twice a day for Day 4 through 7, and then three times daily for Day 8 through 20 in Period 2 |
| PF-07248144 | EXPERIMENTAL | PF-07248144 administered by mouth as a single dose in Period 1 and Period 2. Fluconazole administered by mouth once a day for 13 days in Period 2. |
| PF-07248144 Form 1 (uncoated) Arm | EXPERIMENTAL | Period 1: Participants received Form 1 in a single dose of tablet fasted Period 2: Participants received Form 5 in a single dose of tablet fasted |
| PF-07248144 Form 5 (film-coated) Arm | EXPERIMENTAL | Period 1: Participants received Form 5 in a single dose of tablet fasted Period 2: Participants received Form 1 in a single dose of tablet fasted |
| PF-07248144 Form 5 (film-coated) Adaptive Arm | EXPERIMENTAL | Period 1: Fasted participants received a single dose of tablet of Form 1 orally Period 2: Participants received a single dose of tablet orally of Form 5 in a fed state |
| Name | Type | Description |
|---|---|---|
| PF-07248144 | DRUG | KAT6 inhibitor |
| Fulvestrant | DRUG | Endocrine therapy |
| Everolimus | DRUG | mTOR inhibitor |
| Exemestane | DRUG | Endocrine therapy |
| Letrozole | DRUG | Endocrine Therapy |
| Palbociclib | DRUG | CDK4/6 Inhibitor |
| PF-07220060 | DRUG | CDK4 inhibitor |
| PF-07850327, ARV-471, vepdegestrant | DRUG | PROTAC (PROteolysis Targeting Chimera) ER degrader |
| Itraconazole | DRUG | Participants will receive Itraconazole oral solution once daily on Days 1-12 in Period 2 |
| Oral [14C] PF-07248144 | DRUG | A single oral dose of \[14C\] PF-07248144 will be administered as an extemporaneous suspension in Period 1 |
| Oral unlabeled PF-07248144 | DRUG | A single oral dose of unlabeled PF-07248144 will be administered as tablets in Period 2 |
| IV [14C] PF-07248144 | DRUG | A single IV infusion of \[14C\] PF-07248144 will be administered at the approximate Tmax after administration of the unlabeled oral dose of PF-07248144 in Period 2 |
| Carbamazepine | DRUG | Participants will receive Carbamazepine by mouth once a day for Day 1 through 3, then twice a day for Day 4 through 7, and then three times daily for Day 8 through 20 in Period 2. |
| Fluconazole | DRUG | Fluconazole administered by mouth once a day for 13 days in Period 2. |
Inclusion Criteria: * Confirmed diagnosis of HR-positive HER2-negative breast cancer with evidence of locally advanced or metastatic disease, which is not amenable to surgical resection or radiation therapy with curative intent. * Prior CDK4/6 inhibitor therapy in combination with endocrine therapy...
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PF-07248144 is an investigational small molecule being studied for the treatment of locally advanced or metastatic ER+ HER2- breast cancer. It is also being evaluated in healthy adult participants for pharmacokinetic studies. The drug is currently in Phase 3 clinical development for the breast cancer indication.
PF-07248144 is being developed by Pfizer, Inc., which trades under the ticker symbol PFE on the New York Stock Exchange. Pfizer is conducting clinical trials to evaluate the drug's safety and efficacy in various patient populations.
PF-07248144 is in Phase 3 clinical development for locally advanced or metastatic ER+ HER2- breast cancer. It has completed Phase 1 trials in healthy adults and is also being studied in a Phase 2 trial for advanced or metastatic solid tumors.
PF-07248144 is being studied in several clinical trials. NCT04606446 is a Phase 2 trial in advanced or metastatic solid tumors, including breast, prostate, and lung cancers. NCT07117799, NCT07198035, and NCT07636018 are Phase 1 trials in healthy adults, all of which have been completed.
PF-07248144 is not FDA approved. It is an investigational drug currently in clinical development, with an ongoing Phase 3 trial for locally advanced or metastatic ER+ HER2- breast cancer. The drug has not yet received regulatory approval for any indication.
PF-07248144 is a small molecule being developed by Pfizer for oncology. Its specific molecular target has not been disclosed in the available clinical trial information. The drug is being evaluated for its potential to treat certain types of cancer, including ER+ HER2- breast cancer.