Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as PF-07850327, ARV-471, vepdegestrant
vepdegestrant · 10 trials · 4 indications
It is defined as the number of participants with Grade 4 neutropenia AE (graded by NCI CTCAE v.5.0) with onset within the first 4 cycles divided by the number of participants.
It is defined as the number of participants reducing the dose of palbociclib and/or vepdegestrant due to any cause occurring within the first 4 cycles divided by the number of participants.
It is defined as the number of participants discontinuing palbociclib and/or vepdegestrant due to any cause occurring within the first 4 cycles divided by the number of participants.
Progression-free survival is defined as the time interval from the date of randomization to the date of first documented tumor progression determined by Blinded Independent Central Review (BICR) as per Response Evaluation Criteria in Solid Tumors (RECIST version 1.1) or death due to any cause, whichever come first.
AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).
dn AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞) divided by dose. It is obtained from AUC (0 - t) plus AUC (t - ∞).
dn AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).
AUCinf=area under the plasama concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. It is obtained from AUC (0-t) plus AUC (t-inf)
AUCinf=area under the plasama concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. It is obtained from AUC (0-t) plus AUC (t-inf)
Dose Limiting Toxicities (DLTs) rate for Vepdegestrant in combination with PF-07220060, estimated based on data from DLT-evaluable participants during the DLT observation period (Cycle 1).
Objective response (OR) refers to confirmed complete response (CR) or partial response (PR) according to Response Evaluation Criteria in Solid Tumor (RECIST) version 1.1. as determined by investigator assessment.
Steady-state Area under the plasma concentration versus time curve (AUCtau) of ARV-471 with and without coadministration of samuraciclib
Single dose AUC0-72 of samuraciclib with and without coadministration of ARV 471.
AUCinf was defined as area under the plasma concentration-time curve from time 0 extrapolated to infinity (AUCinf) of ARV-471. AUCinf was calculated by AUClast + (Clast/kel), where Clast was the predicted plasma concentration at the last quantifiable time point from the log-linear regression analysis and kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration time curve.
Cmax was defined as maximum plasma concentration. Cmax of ARV-471 was observed directly from data.
ARV-473 was the epimer of ARV-471. AUC120 was defined as area under the plasma concentrationtime profile from time zero to 120 hours. AUC120 was calculate by Linear/Log trapezoidal method.
ARV-473 was the epimer of ARV-471. Cmax was defined as maximum plasma concentration. Cmax of ARV-473 was observed directly from data.
DLT was defined as any adverse event (AE) or abnormal laboratory value which were related to ARV-471 and assessed as unrelated to disease, disease progression, intercurrent illness or concomitant medications/therapies occurring during the first 28 days of treatment that met at least 1 of the study specified criteria.
| Arm | Type | Description |
|---|---|---|
| Arm A (Investigational Arm) | EXPERIMENTAL | Participants will receive: * Vepdegestrant, orally, once daily, continuously, in a 28-day cycle, plus * Palbociclib, orally, once daily for 21 consecutive days followed by 7 days off treatment in a 28 day cycle |
| Arm B (Comparator Arm): | ACTIVE_COMPARATOR | Participants will receive: * Letrozole, orally, once daily, continuously, in a 28-day cycle, plus * Palbociclib, orally, once daily for 21 consecutive days followed by 7 days off treatment, in a 28-day cycle. |
| Group 1 | EXPERIMENTAL | participants with normal hepatic function |
| Group 2 | EXPERIMENTAL | participants with moderate hepatic impairment |
| Group 3 | EXPERIMENTAL | participants with severe hepatic impairment |
| Vepdegestrant oral and IV administration | EXPERIMENTAL | Participants will receive a single IV infusion of Vepdegestrant on Day 1 of Period 1 followed by a single 200 mg dose of Vepdegestrant registrational tablet on Day 1 of Period 2. |
| vepdegestrant with or without esomeprazole | EXPERIMENTAL | vepdegestrant administered as a single dose in Period 1 and Period 2. Esomeprazole administered once a day for 5 days in Period 2 |
| vepdegestrant in combination with PF-07220060 | EXPERIMENTAL | vepdegestrant administered orally once daily (QD) continuously and PF-07220060 administered orally twice daily (BID) continuously on 28-day cycles |
| Midazolam with and without Vepdegestrant | EXPERIMENTAL | Midazolam administered as a single dose in Period 1 Day 1, and Period 2 Day 1 and Day 15. Vepdegestrant administered once a day for 15 days in Period 2. |
| ARV-471 in combination with Samuraciclib | EXPERIMENTAL | ARV-471 administered orally QD continuously and Samuraciclib administered orally QD continuously on 28-day cycles |
| Vepdegestrant with and without Carbamazepine | EXPERIMENTAL | Vepdegestrant administered as a single dose in Period 1 and Period 2. Carbamazepine administered once a day for 19 days in Period 2. |
| vepdegestrant with and without itraconazole | EXPERIMENTAL | vepdegestrant administered as a single dose in Period 1 and Period 2. Itraconazole administered once a day for 11 days in Period 2. |
| vepdegestrant | EXPERIMENTAL | Daily oral dosages of vepdegestrant |
| Name | Type | Description |
|---|---|---|
| Vepdegestrant (ARV-471/PF-07850327) | DRUG | Pharmaceutical form: Tablets. Route of Administration: Oral |
| Palbociclib | COMBINATION_PRODUCT | Pharmaceutical form: Capsules. Route of Administration: Oral. |
| Letrozole | DRUG | Pharmaceutical form: Capsules. Route of Administration: Orally |
| vepdegestrant | DRUG | Vepdegestrant administered as a single oral 200 mg dose |
| Vepdegestrant (Reference) | DRUG | Participants will receive a single intravenous (IV) dose of Vepdegestrant on Period 1 Day 1 |
| Vepdegestrant (Test) | DRUG | Participants will receive a 200 mg single oral dose of Vepdegestrant tablet formulation on Period 2 Day 1 |
| esomeprazole | DRUG | Experimental treatment to assess an endpoint |
| PF-07220060 | DRUG | Daily oral dosages of PF-07220060 continuously, dose escalation/de-escalation in Phase 1b until recommended phase 2 dose (RP2D) determined, cycles lasting 28 days |
| Midazolam | DRUG | Participants will receive a single dose of Midazolam by mouth in Period 1 Day 1, and Period 2 Day 1 and Day 15 |
| Samuraciclib | DRUG | Daily oral dosages of Samuraciclib continuously, dose escalation/de-escalation in Phase 1b until RP2D determined, cycles lasting 28 days |
| Carbamazepine | DRUG | Participants will receive Carbamazepine by mouth once a day for 19 days in Period 2. |
| Itraconazole | DRUG | Participants will receive itraconazole by mouth once a day for 11 days in Period 2. |
Inclusion Criteria: * Adult participants with loco-regional recurrent or metastatic disease not amenable to curative treatment * Confirmed diagnosis of ER+/HER2- breast cancer * No prior systemic treatment for loco-regional recurrent or metastatic disease * Measurable disease evaluable per Response...
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Vepdegestrant is an investigational small molecule being studied for the treatment of breast cancer, specifically ER+/HER2- locally advanced or metastatic breast cancer. It is also being evaluated in combination with other medicines for advanced or metastatic breast cancer. The drug is currently in clinical development and is not yet approved by the FDA.
Vepdegestrant is a targeted protein degrader that works by targeting the estrogen receptor (ER). It is classified as a SERD, or selective estrogen receptor degrader, which means it binds to the estrogen receptor and promotes its degradation, thereby reducing estrogen signaling in cancer cells.
Vepdegestrant is being developed by Pfizer, Inc., a biopharmaceutical company traded on the New York Stock Exchange under the ticker symbol PFE. The drug is also known by the development codes ARV-471 and PF-07850327.
Vepdegestrant is in Phase 1 clinical development. While one of its trials, NCT05909397, is listed as a Phase 3 study, the overall development program is primarily in Phase 1. The drug is investigational and has not received FDA approval.
Vepdegestrant is being studied in four clinical trials, including NCT05463952 in Japan for ER+/HER2- breast cancer, NCT05909397 comparing vepdegestrant plus palbociclib to letrozole plus palbociclib in advanced breast cancer, NCT06125522 (TACTIVE-U Sub-Study C) in combination with other medicines, and NCT06206837 with PF-07220060 in advanced or metastatic breast cancer.
Yes, Vepdegestrant is the same as ARV-471. It is also known as PF-07850327. These names refer to the same investigational drug being developed by Pfizer for the treatment of breast cancer.