tinlorafenib (PF-07284890) / Pfizer - LARVOL DELTA

Identification of the Clinical Candidate PF-07284890 (ARRY-461), a Highly Potent and Brain Penetrant BRAF Inhibitor for the Treatment of Cancer. (PubMed, J Med Chem) - P1 | "In mice studies, ARRY-461 proved to be highly brain-penetrant and was able to drive regressions of A375 BRAFV600E tumors implanted both subcutaneously and intracranially. Based on compelling preclinical safety and efficacy studies, ARRY-461 was progressed into a Phase 1 A/B clinical trial (NCT04543188)."

Journal • Melanoma • Oncology • Solid Tumor

A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement (clinicaltrials.gov) - P1 | N=65 | Terminated | Sponsor: Pfizer | Trial completion date: Nov 2023 ➔ Mar 2024 | Active, not recruiting ➔ Terminated | Trial primary completion date: Nov 2023 ➔ Mar 2024; Pfizer has made an internal business decision to not continue further development of PF-07284890. This decision was not due to major safety concerns or requests from any regulatory authorities.

Trial completion date • Trial primary completion date • Trial termination • Brain Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Study to Learn About the Study Medicine Called PF-07799544 in People With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=124 | Recruiting | Sponsor: Pfizer | Trial completion date: Dec 2027 ➔ Jun 2027 | Trial primary completion date: Sep 2026 ➔ Jan 2026

Combination therapy • Metastases • Trial completion date • Trial primary completion date • Brain Cancer • CNS Tumor • Colorectal Cancer • Endocrine Cancer • Gastrointestinal Cancer • Glioma • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • BRAF

A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement (clinicaltrials.gov) - P1 | N=56 | Active, not recruiting | Sponsor: Pfizer | Recruiting ➔ Active, not recruiting | N=138 ➔ 56 | Trial completion date: Oct 2024 ➔ Nov 2023 | Trial primary completion date: Oct 2024 ➔ Nov 2023

Enrollment change • Enrollment closed • Trial completion date • Trial primary completion date • Brain Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CYP3A4

A Study to Learn About the Study Medicine Called PF-07799544 in People With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=124 | Recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Metastases • Brain Cancer • CNS Tumor • Colorectal Cancer • Endocrine Cancer • Gastrointestinal Cancer • Glioma • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • BRAF

A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement (clinicaltrials.gov) - P1 | N=138 | Recruiting | Sponsor: Pfizer | N=225 ➔ 138 | Trial completion date: Sep 2023 ➔ Oct 2024 | Trial primary completion date: Sep 2023 ➔ Oct 2024

Enrollment change • Trial completion date • Trial primary completion date • Brain Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CYP3A4

A Study to Learn About the Study Medicine Called PF-07799544 in People With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=124 | Not yet recruiting | Sponsor: Pfizer | Trial primary completion date: May 2026 ➔ Aug 2026

Combination therapy • Trial primary completion date • Brain Cancer • CNS Tumor • Colorectal Cancer • Endocrine Cancer • Gastrointestinal Cancer • Glioma • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • BRAF

A Study to Understand the Effect of Low-Fat and High-Fat Meals on the Medicine Called PF-07284890 in Healthy Adults (clinicaltrials.gov) - P1 | N=12 | Completed | Sponsor: Pfizer | Recruiting ➔ Completed

Trial completion

A Study to Learn About the Study Medicine Called PF-07799544 in People With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=124 | Not yet recruiting | Sponsor: Pfizer

Combination therapy • New P1 trial • Brain Cancer • Colorectal Cancer • Endocrine Cancer • Gastrointestinal Cancer • Glioma • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • BRAF

A Study to Understand the Effect of Low-Fat and High-Fat Meals on the Medicine Called PF-07284890 in Healthy Adults (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Recruiting

Enrollment open

A Study to Understand the Effect of Low-Fat and High-Fat Meals on the Medicine Called PF-07284890 in Healthy Adults (clinicaltrials.gov) - P1 | N=12 | Not yet recruiting | Sponsor: Pfizer

New P1 trial

[VIRTUAL] Trial in progress: Phase 1a/b study of PF-07284890 (brain-penetrant BRAF inhibitor) with/without binimetinib in patients with BRAF V600-mutant solid tumors. (ASCO 2021) - P1 | "Cohort 6 (̃10 pts) will assess the effect of PF-07284890 + binimetinib on CYP3A activity using midazolam as a substrate . For both Phase 1a and 1b, Tx will continue until disease progression, unacceptable toxicity or patient refusal . Study began enrolling pts in January 2021 and is ongoing."

Clinical • P1 data • Brain Cancer • CNS Disorders • Immunology • Oncology • Solid Tumor

[VIRTUAL] Nonclinical development of PF-07284890 (ARRY-461), a potent, brain-penetrant, small molecule inhibitor of BRAF V600-mutation-driven tumors in vitro and in vivo (AACR 2021) - "GLP safety studies demonstrated a good safety profile for PF-07284890. PF‑07284890 is fully brain penetrant, with the potential to address this key unmet medical need and thereby defines a new class of brain penetrant, potent and selective BRAF inhibitors."

Preclinical • Melanoma • Oncology • Solid Tumor • BRAF

A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement (clinicaltrials.gov) - P1; N=225; Recruiting; Sponsor: Pfizer; Not yet recruiting ➔ Recruiting; Trial completion date: May 2023 ➔ Sep 2023; Initiation date: Sep 2020 ➔ Jan 2021; Trial primary completion date: May 2023 ➔ Sep 2023

Clinical • Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date • Brain Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CYP3A4

A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement (clinicaltrials.gov) - P1; N=225; Not yet recruiting; Sponsor: Pfizer

Clinical • New P1 trial • Brain Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor