WATERTOWN, Mass.– Treeline Biosciences today announced the initiation of Phase 1 clinical trials for three oncology programs and the close of a $200 million Series A extension, bringing the company’s total funding to $1.1 billion.
The trials include two internally developed programs — TLN-121, a BCL6 degrader, and TLN-372, a pan-KRAS inhibitor — along with TLN-254, an in-licensed EZH2 inhibitor. TLN-121 and TLN-254 are being studied in patients with lymphoma, while TLN-372 is enrolling patients with cancers that carry KRAS mutations.
“We aspire to create the next great enduring biopharma company,” said Josh Bilenker, M.D., Co-founder and CEO of Treeline. “Our funding mandate has allowed us to recruit proven scientists, rigorously test assumptions, and curate a pipeline through parallel discovery efforts. BCL6 and KRAS are formidable targets, requiring novel chemistry and assay development. We hope these programs deliver for patients and create momentum for our next clinical entries.”
Treeline was co-founded by Bilenker, who previously founded Loxo Oncology, and Jeff Engelman, M.D., Ph.D., the company’s Chief Scientific Officer and former director of thoracic oncology at Massachusetts General Hospital. The company’s internal R&D team uses advanced computational tools to accelerate discovery and development across cancer, neurological, and autoimmune diseases. Its pipeline spans small molecules, degraders, molecular glues, and targeted therapy antibody-drug conjugates, designed with scale and longevity in mind.
The company’s first three clinical programs reflect its founding team’s extensive experience in oncology. TLN-121 targets BCL6, a protein that certain lymphoma cells use to silence genes blocking growth and survival. By degrading BCL6, the therapy aims to reduce toxicity and potentially allow for use alongside existing lymphoma treatments. TLN-372 is being studied in patients with KRAS-altered solid tumors, addressing a target that is implicated in roughly one in four adult cancers. While FDA-approved medicines exist for the G12C variant, other KRAS mutations remain unaddressed, and TLN-372 was designed for sustained, pan-KRAS inhibition. TLN-254, a small molecule EZH2 inhibitor in-licensed after Phase 2 testing in refractory lymphoma, is now enrolling patients with peripheral and cutaneous T-cell lymphomas.
Treeline’s $200 million Series A extension was supported by AI Life Sciences, an affiliate of Access Industries, ARCH Venture Partners, OrbiMed, GV, KKR, T. Rowe Price Associates, Ajax Health/Zeus, Casdin Capital, Fidelity Management & Research Company, Aisling Capital, Rock Springs Capital, and Exor.
“Our team and pipeline are built for scaled invention and long-term impact,” said Engelman. “With these first clinical trials, Treeline is moving one step closer to translating discovery into transformative therapies for patients.”
