CDK2 inhibitors(Cyclin-dependent kinase 2 inhibitors), CDK4 inhibitors(Cyclin-dependent kinase 4 inhibitors), CDK6 inhibitors(Cyclin-dependent kinase 6 inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [3]

Active Indication

Fallopian Tube CarcinomaHormone receptor positive HER2 negative breast cancerMale Breast Neoplasms+ [3]

Inactive Indication-

Originator Organization

Pfizer Inc.

Active Organization

Pfizer Inc.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Structure

Molecular FormulaC20H27F2N5O4S

InChIKeyQIEKHLDZKRQLLN-FOIQADDNSA-N

CAS Registry2185857-97-8

Clinical Trials associated with PF-06873600

NCT03519178 / Active, not recruitingPhase 2

PHASE 1/2A DOSE ESCALATION AND EXPANSION STUDY EVALUATING SAFETY, TOLERABILITY, PHARMACOKINETIC, PHARMACODYNAMICS AND ANTI-TUMOR ACTIVITY OF PF-06873600 AS A SINGLE AGENT AND IN COMBINATION WITH ENDOCRINE THERAPY

The purpose of this clinical trial is to learn about the safety and effects of study medicine (PF-06873600) when taken alone or with hormone therapy by people with cancer.
People may be able to participate in this study if they have the following types of cancer: Hormone Receptor positive (HR+) breast cancer; Human Epidermal Growth Factor Receptor 2 (HER2)-negative breast cancer that is advanced or metastatic (spread to other parts of the body); triple negative breast cancer; epithelial ovarian cancer; fallopian tube cancer; or primary peritoneal cancer.
All participants in this study will receive the study medicine by mouth, 1 to 2 times a day at home. The dose of the study medicine may be changed during the study.
Some participants will also receive hormone therapy. The hormone therapy will be either letrozole by mouth once a day at home, or fulvestrant as a shot into the muscle. Fulvestrant will be given every two weeks at the study clinic for the first month, and then once a month after that.
Participants will take part in this study for at least 7 to 8 months, depending on how they respond to the therapy. During this time participants will visit the study clinic once a week.

Start Date07 Mar 2018

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with PF-06873600

100 Translational Medicine associated with PF-06873600

100 Patents (Medical) associated with PF-06873600

Literatures (Medical) associated with PF-06873600

15 May 2023·Bioorganic & medicinal chemistry letters

Synthesis and biological evaluation of novel pteridin-7(8H)-one derivatives as potent CDK2 inhibitors.

Article

Author: Wang, Xia ; Yuan, Xin ; Jiang, Hongyu ; Ding, Lei ; Xiang, Lianghua ; Tang, Chunlei

Cyclin-dependent kinase 2 (CDK2) is considered as an important target in the research of antitumor drugs. Taking the CDK2/4/6 inhibitor Ebvaciclib as the positive control and an in-house library compound (23) as the lead compound, three classes of 30 target compounds with pteridin-7(8H)-one as the core structure were designed to establish structure-activity relationships (SAR). In general, SAR of pteridin-7(8H)-one CDK2 inhibitors is systematically described in this paper, resulting in the discovery of two compounds (KII-17 and KII-21) with further research value. After the above compounds were tested for CDK2/4/6 kinase selectivity, we found that compound KII-21 was about 3 and 4 times more selective to CDK2-cyclinE2 than CDK4-cyclinD1 and CDK6-cyclinD3, respectively. This work also provides a reference basis for the subsequent research on CDK2 inhibitors.

01 Oct 2021·Cancer cellQ1 · MEDICINE

Restoring order at the cell cycle border: Co-targeting CDK4/6 and CDK2

Q1 · MEDICINE

Article

Author: Schiff, Rachel ; Grinshpun, Albert ; Jeselsohn, Rinath

Overcoming resistance to CDK4/6 inhibitors is a major clinical challenge. In this issue of Cancer Cell, Freeman-Cook et al. study mechanisms of resistance to CDK4/6 inhibitors by employing a CRISPRa screen. They identify the cyclin E-CDK2 axis and Myc signaling as key pathways of resistance and develop PF-06873600, a selective CDK2/4/6 inhibitor.

01 Oct 2021·Cancer cellQ1 · MEDICINE

Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor

Q1 · MEDICINE

Article

Author: Chionis, John ; Lapek, John ; Costa-Jones, Cinthia ; Boras, Britton ; Miller, Nichol ; Zhang, Cathy ; Salek-Ardakani, Shahram ; Kan, Zhengyan ; Weinrich, Scott L ; Eisele, Koleen ; Ornelas, Martha A ; Zhu, Zhou ; Zhang, Qin ; McTigue, Michele ; White, Michael A ; He, You-Ai ; Almaden, Jonathan ; Ding, Ying ; McMillan, Elizabeth ; Hoffman, Robert L ; Wei, Ping ; VanArsdale, Todd ; Oderup, Cecilia ; Zehnder, Luke R ; Kephart, Susan E ; Mu, Xinmeng Jasmine ; Wilson, Elizabeth ; Sutton, Scott ; Wang, Tim S ; Behenna, Douglas ; Liu, Chaoting ; Lee, Nathan ; Tran, Khanh T ; Ninkovic, Sacha ; Nagata, Asako ; Ferre, Rose Ann ; Murray, Brion ; Bienkowska, Jadwiga R ; Freeman-Cook, Kevin ; Carelli, Jordan ; Looper, David ; Solowiej, James E ; Niessen, Sherry ; Huser, Nanni ; Nguyen, Lisa ; Xu, Meirong ; Dann, Stephen G ; Visswanathan, Ravi

The CDK4/6 inhibitor, palbociclib (PAL), significantly improves progression-free survival in HR⁺/HER2^- breast cancer when combined with anti-hormonals. We sought to discover PAL resistance mechanisms in preclinical models and through analysis of clinical transcriptome specimens, which coalesced on induction of MYC oncogene and Cyclin E/CDK2 activity. We propose that targeting the G₁ kinases CDK2, CDK4, and CDK6 with a small-molecule overcomes resistance to CDK4/6 inhibition. We describe the pharmacodynamics and efficacy of PF-06873600 (PF3600), a pyridopyrimidine with potent inhibition of CDK2/4/6 activity and efficacy in multiple in vivo tumor models. Together with the clinical analysis, MYC activity predicts (PF3600) efficacy across multiple cell lineages. Finally, we find that CDK2/4/6 inhibition does not compromise tumor-specific immune checkpoint blockade responses in syngeneic models. We anticipate that (PF3600), currently in phase 1 clinical trials, offers a therapeutic option to cancer patients in whom CDK4/6 inhibition is insufficient to alter disease progression.

100 Deals associated with PF-06873600

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fallopian Tube Carcinoma	Phase 2	US	Pfizer Inc.	07 Mar 2018
Fallopian Tube Carcinoma	Phase 2	JP	Pfizer Inc.	07 Mar 2018
Fallopian Tube Carcinoma	Phase 2	BG	Pfizer Inc.	07 Mar 2018
Fallopian Tube Carcinoma	Phase 2	CA	Pfizer Inc.	07 Mar 2018
Fallopian Tube Carcinoma	Phase 2	RU	Pfizer Inc.	07 Mar 2018
Fallopian Tube Carcinoma	Phase 2	UA	Pfizer Inc.	07 Mar 2018
Hormone receptor positive HER2 negative breast cancer	Phase 2	US	Pfizer Inc.	07 Mar 2018
Hormone receptor positive HER2 negative breast cancer	Phase 2	JP	Pfizer Inc.	07 Mar 2018
Hormone receptor positive HER2 negative breast cancer	Phase 2	BG	Pfizer Inc.	07 Mar 2018
Hormone receptor positive HER2 negative breast cancer	Phase 2	CA	Pfizer Inc.	07 Mar 2018

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03519178 (Part 1, SABCS2022)	Phase 1/2	Ovarian Cancer HR+ \| HER2- \| TNBC ... View more	67	PF-3600 alone	txparqlcws(oiglwhmpdv) = The most frequently reported treatment-related AEs (all grade/grade ≥3) for PF-3600 alone and PF-3600 + F, respectively, were nausea (50%/0% and 67%/0%), anemia (38%/14% and 44%/11%) and neutropenia (29%/16% and 22%/11%) suikyoqilv (ktxnmofajw )	Positive	15 Feb 2022
				PF-3600 + F

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