^
    17d
    18F-FLT PET, a Non-Invasive Pharmacodynamic Biomarker of Tumor Cell Proliferation, Detected Differential Response to Various Cyclin Dependent Kinase (CDK) Inhibitors. (PubMed, Mol Cancer Ther)
    Consistent with this observation, 18F-FLT PET was able to differentiate the resistance to Palbociclib from sensitivity to PF-06873600 (CDK2/4/6 inhibitor) and PF-07104091 in OVCAR-3 model. This work highlights the utility of 18F-FLT PET as a quantitative, non-invasive biomarker which provides whole-body information. 18F-FLT PET has potential to be a biomarker in novel CDK inhibitor clinical trials to evaluate Palbociclib resistance and identifying responding and non-responding patients.
    PK/PD data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • ebvaciclib (PF-06873600) • tagtociclib (PF-07104091)
    1m
    Individualized Pooled CRISPR/Cas9 Screenings Identify CDK2 as a Druggable Vulnerability in a Canine Mammary Carcinoma Patient. (PubMed, Vet Sci)
    A comparison of essential genes for tumor cells survival identified CDK2 as a functional vulnerability in canine mammary tumors (CMTs) that can be targeted with the PF3600 inhibitor. Additional potential targets were also uncovered, providing insights for personalized cancer treatments in dogs.
    Journal
    |
    CDK2 (Cyclin-dependent kinase 2)
    |
    ebvaciclib (PF-06873600)
    2ms
    C3661001: A Study of PF-06873600 in People With Cancer (clinicaltrials.gov)
    P1/2, N=155, Terminated, Pfizer | Phase classification: P2 --> P1/2 | Active, not recruiting --> Terminated; Per business decision, but not due to safety concerns or regulatory request.
    Phase classification • Trial termination
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    almost2years
    Discovery of targeted therapies for cancer patients: CDK2/4/6 inhibitor Ebvaciclib and EZH2 inhibitor PF-06821497 (ACS-Fall 2023)
    Ebvaciclib, is a CDK2/4/6 inhibitor designed to be co-dosed with hormone therapy (letrozole or fulvestrant) to treat HR+ breast cancer. PF-06821497 is an EZH2 inhibitor currently being evaluated alone and in combination with enzalutamide to treat patients with castration resistant prostate cancer who have received either abiraterone and/or enzalutamide treatment and have evidence of prostate cancer progression. Discovery, synthesis, and early clinical results will be presented.
    Clinical
    |
    Xtandi (enzalutamide) • abiraterone acetate • fulvestrant • letrozole • ebvaciclib (PF-06873600) • mevrometostat (PF-06821497)
    2years
    C3661001: A Study of PF-06873600 in People With Cancer (clinicaltrials.gov)
    P2, N=155, Active, not recruiting, Pfizer | Trial completion date: Apr 2023 --> Nov 2024
    Trial completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over2years
    C3661001: A Study of PF-06873600 in People With Cancer (clinicaltrials.gov)
    P2, N=155, Active, not recruiting, Pfizer | Trial completion date: Jan 2024 --> Apr 2023
    Trial completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over2years
    C3661001: A Study of PF-06873600 in People With Cancer (clinicaltrials.gov)
    P2, N=155, Active, not recruiting, Pfizer | N=69 --> 155
    Enrollment change • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over2years
    C3661001: A Study of PF-06873600 in People With Cancer (clinicaltrials.gov)
    P2, N=69, Active, not recruiting, Pfizer | Recruiting --> Active, not recruiting | N=160 --> 69 | Trial completion date: Oct 2025 --> Jan 2024
    Enrollment closed • Enrollment change • Trial completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over3years
    Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor. (PubMed, Cancer Cell)
    The CDK4/6 inhibitor, palbociclib (PAL), significantly improves progression-free survival in HR/HER2 breast cancer when combined with anti-hormonals...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...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.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Ibrance (palbociclib) • ebvaciclib (PF-06873600)
    almost4years
    Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer. (PubMed, J Med Chem)
    Further, we detail the use of molecular dynamics simulations to provide insights into the basis for selectivity against CDK9. Based on overall potency, selectivity, and ADME profile, PF-06873600 (22) was identified as a candidate for the treatment of cancer and advanced to phase 1 clinical trials.
    Journal
    |
    CDK9 (Cyclin Dependent Kinase 9)
    |
    ebvaciclib (PF-06873600)
    4years
    A Safety, Pharmacokinetic, Pharmacodynamic and Anti-Tumor Study of PF-06873600 as a Single Agent and in Combination With Endocrine Therapy (clinicaltrials.gov)
    P2, N=157, Recruiting, Pfizer | Trial completion date: May 2024 --> Jul 2025 | Trial primary completion date: Nov 2022 --> Feb 2023
    Clinical • Trial completion date • Trial primary completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over4years
    A Safety, Pharmacokinetic, Pharmacodynamic and Anti-Tumor Study of PF-06873600 as a Single Agent and in Combination With Endocrine Therapy (clinicaltrials.gov)
    P2, N=220, Recruiting, Pfizer | Trial completion date: Apr 2026 --> May 2024 | Trial primary completion date: Nov 2023 --> Nov 2022
    Clinical • Trial completion date • Trial primary completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over4years
    A Safety, Pharmacokinetic, Pharmacodynamic and Anti-Tumor Study of PF-06873600 as a Single Agent and in Combination With Endocrine Therapy (clinicaltrials.gov)
    P2, N=220, Recruiting, Pfizer | Trial completion date: Nov 2023 --> Apr 2026
    Clinical • Trial completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)
    over4years
    A Safety, Pharmacokinetic, Pharmacodynamic and Anti-Tumor Study of PF-06873600 as a Single Agent and in Combination With Endocrine Therapy (clinicaltrials.gov)
    P2, N=220, Recruiting, Pfizer | Trial completion date: Mar 2023 --> Nov 2023 | Trial primary completion date: Mar 2023 --> Nov 2023
    Clinical • Trial completion date • Trial primary completion date • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HR positive • HER-2 negative
    |
    ebvaciclib (PF-06873600)