Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as PF-07220060 CDK4 inhibitor, Atirmociclib
PF-07220060 · 7 trials · 8 indications
Time from the date of randomization to the date of the first documentation of objective progressive disease as determined by blinded independent central review (BICR) per RECIST v1.1, or death due to any cause, whichever occurs first
CCCA was determined by antigen Kiel 67 (Ki-67) value as decided by Sponsor. Ki-67 was extensively used as a prognostic and predictive biomarker for cancer diagnosis and treatment. Ki-67 expression was measured by immunohistochemistry. Assessment at Day 14 was done in blinded manner by centrally assessed biopsy.
First cycle (28 days) dose limiting toxicities (Parts 1A, 1B, 1C, 1F)
Adverse Events
safety laboratory abnormalities
vital signs and heart rate corrected QT interval
Maximal Concentration, Time to Maximum Plasma Concentration, Area under the Plasma Concentration (Part 1D)
Maximal Concentration, Time to Maximum Plasma Concentration, Area under the Plasma Concentration (Part 1E)
AUClast was area under the plasma concentration time-curve from zero (pre-dose) to the last measured concentration (If data does not permit reporting of AUCinf). The geometric coefficient of variation is expressed in percentage. The ratio (Test/Reference) of adjusted means and 90% CI are then expressed as percentages.
AUCinf was area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf , if data permits). It is obtained from AUC (0-t) plus AUC (t-inf). The geometric coefficient of variation is expressed in percentage. The ratio (Test/Reference) of adjusted means and 90% CI are then expressed as percentages.
Cmax was the maximum observed plasma concentration directly observed from data. The geometric coefficient of variation is expressed in percentage. The ratio (Test/Reference) of adjusted means and 90% CI are then expressed as percentages.
Percentage of 14C excreted in urine following 14C PF-07220060 dose administration was determined as: (total 14C urine/ 14C dose administered)\*100 where, 14C dose was administered dose of 14C PF-07220060.
Percentage of 14C excreted in feces following 14C PF-07220060 oral dose administration was determined as: (total 14C feces/ 14C oral dose administered)\*100 where, 14C dose was administered dose of 14C PF-07220060.
Percentage recovery of total radioactivity (14C ) in urine and feces was determined based on total administered dose.
The percentage of five major metabolites detected in plasma after oral administration of PF-07220060: 480a, 480b, 496a, M3 and 496b are reported in this outcome measure. The processed samples were analyzed by liquid chromatography mass spectrometry- accelerator mass spectrometry (LC-MS-AMS). For calculation of metabolite percentage of total plasma radioactivity (RA), first composite time-normalized human plasma pools were prepared for each participant from plasma samples collected from 0-96 hours post-dose (i.e., a hamilton pool). Next, a multi-subject pool was created by combining equal volumes of each of the above individual participant pools. Results presented here are the single value output from these individual pooled multi-subject time-normalized samples.
The percentage of five major metabolites detected in urine after oral administration of PF-07220060: 480a, 480b, 496a, M3 and 496b are reported in this outcome measure. The processed samples were analyzed by LC-MS-AMS. For calculation of percentage of metabolites, first composite time-normalized human urine pools were prepared for each participant from urine samples collected from 0-144 hours post-dose (i.e., a hamilton pool). Next, a multi-subject pool was created by combining equal volumes of each of the above individual participant pools. Results presented here are the single value output from these individual pooled multi-subject time-normalized samples.
The percentage of five major metabolites detected in feces after oral administration of PF-07220060: 480a, 480b, 496a, M3 and 496b are reported in this outcome measure. The processed samples were analyzed by LC-MS-AMS. For calculation of percentage of metabolites, first composite time-normalized human fecal homogenate pools were prepared for each participant from fecal samples collected from 0-196 hours post-dose (i.e., a hamilton pool). Next, a multi-subject pool was created by combining equal volumes of each of the above individual participant pools. Results presented here are the single value output from these individual pooled multi-subject time-normalized samples.
The percentage of five major metabolites detected in feces after IV administration of PF-07220060: 480a, 480b, 496a, M3 and 496b are reported in this outcome measure. The processed samples were analyzed by LC-MS-AMS. For calculation of percentage of metabolites, first composite time-normalized human fecal homogenate pools were prepared for each participant from fecal samples collected from 0-196 hours post-dose (i.e., a hamilton pool). Next, a multi-subject pool was created by combining equal volumes of each of the above individual participant pools. Results presented here are the single value output from these individual pooled multi-subject time-normalized samples.
| Arm | Type | Description |
|---|---|---|
| Arm A | EXPERIMENTAL | PF-07220060 tablet taken by mouth plus Letrozole tablet taken by mouth |
| Arm B | ACTIVE_COMPARATOR | Investigator's Choice of CDK4/6 inhibitor (tablet/capsule) taken by mouth with letrozole tablet taken by mouth |
| Arm A/Experimental/PF-07220060 plus letrozole | EXPERIMENTAL | PF-07220060 given as tablet by mouth twice a day for 14 days. Letrozole given as tablet by mouth once a day for 14 days. |
| Arm B/Control/letrozole | ACTIVE_COMPARATOR | Letrozole given by mouth once a day for 14 days. |
| 1A Monotherapy Escalation Arm 1 | EXPERIMENTAL | PF-07220060 Monotherapy Escalation |
| 1A Monotherapy Escalation Arm 2 | EXPERIMENTAL | PF-07220060 Monotherapy Escalation |
| 1A Monotherapy Escalation Arm 3 | EXPERIMENTAL | PF-07220060 Monotherapy Escalation |
| 1A Monotherapy Escalation Arm 4 | EXPERIMENTAL | PF-07220060 Monotherapy Escalation |
| 1B Combination Dose Finding Arm 1 | EXPERIMENTAL | PF-07220060 with Letrozole combination Escalation |
| 1B Combination Dose Finding Arm 2 | EXPERIMENTAL | PF-07220060 with Letrozole Combination Escalation |
| 1C Combination Dose Finding Arm 1 | EXPERIMENTAL | PF-07220060 with Fulvestrant Combination Escalation |
| 1C Combination Dose Finding Arm 2 | EXPERIMENTAL | PF-07220060 with Fulvestrant Combination Escalation |
| 2B Combination Dose Expansion | EXPERIMENTAL | PF-07220060 with Letrozole Combination Expansion |
| 2C Combination Dose Expansion | EXPERIMENTAL | PF-07220060 with fulvestrant Combination Expansion |
| 1D Monotherapy Food Effect | EXPERIMENTAL | PF-07220060 Monotherapy Food Effect |
| 1A Monotherapy Escalation Arm 5 | EXPERIMENTAL | PF-07220060 Monotherapy Escalation |
| 1F Combination Dose Finding | EXPERIMENTAL | PF-07220060 with Enzalutamide Escalation |
| 1E DDI Cohort | EXPERIMENTAL | PF-07220060 DDI with Midazolam |
| 2D Combination Dose Expansion | EXPERIMENTAL | PF-07220060 with enzalutamide Combination Expansion |
| 2A Combination Dose Expansion | EXPERIMENTAL | PF-07220060 with fulvestrant combination dose expansion |
| 2E Combination Dose Expansion | EXPERIMENTAL | PF-07220060 Monotherapy OR PF-07220060 plus fulvestrant combination therapy |
| Cohort 1, Period 1: PF-07220060 | EXPERIMENTAL | In Cohort 1, Period 1 participants will receive a single dose of PF-07220060 tablet given orally and administered with food on Day 1. |
| Cohort 1, Period 2: PF-07220060 and itraconazole | EXPERIMENTAL | In Cohort 1 Period 2, participants will receive oral dose of itraconazole once daily from Day 1 to Day 9. On the morning of Day 4, participants will first receive one oral dose of itraconazole followed by a single oral dose of PF-07220060 tablet |
| Cohort 2, Period 1: PF-07220060 | EXPERIMENTAL | In Cohort 2, Period 1 participants will receive a single dose of PF-07220060 tablet given orally and administered with food on Day 1. |
| Cohort 2, Period 2: PF-07220060 probenecid | EXPERIMENTAL | In Cohort 2, Period 2, participants will receive oral dose of probenecid four times a day from Day 1 to Day 9. On the morning of Day 3, participants will first receive one oral dose of probenecid followed by a single oral dose of PF-07220060 tablet. |
| Regimen A; Treatment Sequence A | EXPERIMENTAL | Single Oral Dose of reference tablet formulation PF-07220060, then at least 7 day washout, followed by a single oral dose of test tablet formulation PF-07220060 |
| Regimen B; Treatment Sequence B | EXPERIMENTAL | Single Oral Dose of test tablet formulation PF-07220060, then at least 7 day washout, followed by a single oral dose of reference tablet formulation PF-07220060 |
| Period 1 | EXPERIMENTAL | Single dose PF-07220060 alone |
| Period 2 | EXPERIMENTAL | Single dose PF-07220060 given after multiple doses of carbamazepine |
| Cohort 1 | EXPERIMENTAL | Participants will receive one dose of \[14C\] PF-07220060 by mouth |
| Cohort 2 | EXPERIMENTAL | Participants will take one dose of PF-07220060 by mouth and one dose as an IV (intravenous) infusion of \[14C\] PF-07220060. |
| Name | Type | Description |
|---|---|---|
| PF-07220060 | DRUG | CDK4 inhibitor |
| letrozole | DRUG | endocrine therapy |
| abemaciclib | DRUG | CDK4/6 inhibitor |
| palbociclib | DRUG | CDK4/6 inhibitor |
| ribociclib | DRUG | CDK4/6 inhibitor |
| Fulvestrant | COMBINATION_PRODUCT | Endocrine Therapy |
| Midazolam | DRUG | Benzodiazepine used for DDI |
| Enzalutamide | COMBINATION_PRODUCT | Androgen Receptor inhibitor |
| Itraconazole | DRUG | Capsule given orally |
| Probenecid | DRUG | Tablet given orally |
| Carbamazepine ER Tablet | DRUG | Carbamazepine dosing titration regimen in Period 2 from Day 1 to 18 |
| Oral [14C]PF-07220060 | DRUG | A single oral dose of \[14C\]PF-07220060, will be administered as a liquid formulation in Cohort 1. |
| Oral PF-07220060 | DRUG | A single oral dose of PF-07220060, will be administered as a liquid formulation in Cohort 2. |
| IV [14C] PF-07220060 | DRUG | A single IV infusion of \[14C\]PF-07220060 will be administered in Cohort 2 at Tmax after the administration of the unlabeled oral dose. |
Inclusion Criteria: * Histological confirmation of breast cancer with evidence of locally advanced or metastatic disease, which is not amenable to surgical resection or radiation therapy with curative intent. * Documented estrogen receptor (ER) and/or progesterone receptor (PR)-positive tumor * Doc...
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Atirmociclib is an investigational small molecule being studied for the treatment of breast cancer, including advanced or metastatic breast cancer. It is also being evaluated in healthy participants for pharmacokinetic studies and in participants with hepatic impairment. The drug is currently in clinical development and has not been approved by regulatory authorities.
Atirmociclib is a CDK inhibitor, belonging to the -ciclib class of drugs that target cyclin-dependent kinases. Specifically, it is a CDK4 inhibitor, which means it works by inhibiting CDK4, a key regulator of cell cycle progression. This mechanism is being studied in the context of hormone receptor-positive breast cancer.
Atirmociclib is being developed by Pfizer, Inc., a multinational pharmaceutical company listed on the New York Stock Exchange under the ticker symbol PFE. Pfizer is conducting clinical trials to evaluate the safety, tolerability, and efficacy of Atirmociclib in various patient populations.
Atirmociclib is in Phase 1 clinical development. While some completed trials were Phase 1 and Phase 2, the most advanced ongoing trial is a Phase 3 study. However, the drug is still investigational and has not received FDA approval. It remains in active clinical development across multiple studies.
Atirmociclib has been studied in several clinical trials. NCT06267963 was a Phase 1 study in healthy adults, NCT06465368 was a Phase 2 study in postmenopausal women with breast cancer, NCT06760637 is an active Phase 3 study in HR-positive HER2-negative breast cancer, and NCT07130097 was a Phase 1 study comparing tablet formulations in healthy participants.
Yes, Atirmociclib is also known as PF-07220060. The drug is referred to by both names in clinical trial registries and scientific literature. Researchers and clinicians may use either name when discussing the drug, and both refer to the same investigational CDK4 inhibitor being developed by Pfizer.