Treeline Biosciences (or Treeline) today announced the initiation of Phase 1 trials for two internally discovered programs, TLN-121 and TLN-372, and a third in-licensed program, TLN-254. TLN-121, a BCL6 degrader, and TLN-254, an EZH2 inhibitor, are both being studied in patients with lymphoma. TLN-372, a pan-KRAS inhibitor, is being studied in patients with cancers expressing certain KRAS mutations. The company also announced the close of a $200 million Series A extension, bringing total funding to $1.1 billion.

This press release features multimedia. View the full release here: https://www.businesswire.com/news/home/20250903916944/en/

Treeline CEO and Co-Founder Josh Bilenker, M.D., and CSO and Co-Founder Jeff Engelman, M.D. Ph.D.

“We aspire to create the next great enduring biopharma company,” said Josh Bilenker, M.D., Treeline’s Co-Founder and CEO. “Our funding mandate has allowed us to recruit proven scientists, rigorously test assumptions and curate a pipeline from parallel discovery efforts. BCL6 and KRAS are formidable targets that required difficult chemistry and novel assay development. We hope these programs deliver for patients and create momentum for our next set of clinical entries."

Go here to read more of Josh’s perspective on today’s news.

Treeline Facts

• Co-founded by CEO Josh Bilenker and CSO Jeff Engelman, both oncologists with experience leading R&D teams. Josh previously founded Loxo Oncology, which developed three FDA-approved medicines. Jeff was director of thoracic oncology at Massachusetts General Hospital and later global head of oncology at the Novartis Institutes for BioMedical Research.
• Internal R&D team uses leading-edge computational tools to prioritize workflow and accelerate timelines.
• Therapeutic areas include cancer, neurological and autoimmune diseases.
• Programs include small molecules, degraders and glues, and targeted therapy ADCs (TT-ADCs).
• Team and pipeline were built for scaled invention and company longevity.
• $1.1 billion raised to-date, including a recent $200M Series A extension; investors include: AI Life Sciences, an affiliate of Access Industries; ARCH Venture Partners; OrbiMed; GV; KKR; accounts advised by T. Rowe Price Associates, Inc.; Ajax Health/Zeus; Casdin Capital; Fidelity Management & Research Company; Aisling Capital; Rock Springs Capital; and Exor.

Medicines in the Making

Treeline’s founding team has worked extensively in cancer R&D, and its first three clinical programs reflect this hard-won experience:

TLN-121 — BCL6 Protein Degrader for Lymphomas

BCL6 is a naturally occurring protein that certain lymphoma cells exploit to silence genes that would otherwise block their growth and survival. TLN-121 is a protein degrader designed to remove BCL6 from cancer cells while avoiding off-target effects that could cause toxicity, potentially enabling combination use with standard-of-care lymphoma therapies. The Phase 1 trial (NCT07082803) is enrolling patients with B-cell and T-cell lymphomas.

TLN-372 — Pan-KRAS Inhibitor for Solid Tumors

Approximately one in four adult cancers harbor a KRAS alteration. While there are FDA-approved medicines for G12C mutations, other KRAS variants remain unaddressed by targeted therapies. TLN-372 is a small molecule inhibitor with novel chemistry designed for deep, continuous pan-KRAS inhibition, and possesses favorable drug-like properties. The Phase 1 trial will enroll patients with KRAS-altered solid tumors.

TLN-254 — EZH2 Inhibitor for Lymphomas

EZH2 regulates gene expression and is often overexpressed or mutated in cancers. TLN-254 is a small molecule inhibitor that was in-licensed after Phase 2 testing in refractory lymphoma. The Phase 1 trial (NCT06733441) is enrolling patients with peripheral and cutaneous T-cell lymphomas.

About Treeline

Treeline Biosciences, Inc. (or Treeline) is a privately held, clinical-stage biopharma company that aspires to make medicines at the highest level. We match compelling disease targets with proven drug approaches, by integrating in-house R&D with leading-edge computational tools. We choose programs with the potential to redefine the treatment of cancer and other serious diseases. We are led by a team of biology, chemistry, protein science, computation, and clinical development leaders working across the U.S. and Europe. You can learn more about our clinical trials here and more about our company here.

View source version on businesswire.com: https://www.businesswire.com/news/home/20250903916944/en/