Treeline Biosciences Secures $200M Series A Extension to Advance Phase 1 Clinical Trials

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Treeline Biosciences, a biotechnology company based in Watertown, Massachusetts, has announced the initiation of Phase 1 clinical trials for three of its drug candidates and the closing of a $200 million Series A extension. This funding brings the company’s total capital raised to approximately $1.1 billion.

The three programs entering clinical trials are TLN-121, TLN-372, and TLN-254. TLN-121 is a BCL6 degrader being studied in patients with lymphoma, while TLN-254 is an EZH2 inhibitor, also targeting lymphoma patients. TLN-372 is a pan-KRAS inhibitor designed for cancers expressing certain KRAS mutations. The company has disclosed that TLN-121 and TLN-372 are internally developed, whereas TLN-254 was licensed from Hengrui Pharmaceuticals in 2023 for $11 million upfront, with up to $695 million in potential milestones.

Treeline was founded in early 2021 by Josh Bilenker, M.D., and Jeff Engelman, M.D., Ph.D., both oncologists with experience leading R&D teams. Bilenker previously founded Loxo Oncology, which developed three FDA-approved medicines, and Engelman served as director of thoracic oncology at Massachusetts General Hospital and later global head of oncology at the Novartis Institutes for BioMedical Research. The company’s internal R&D team utilizes leading-edge computational tools to prioritize workflow and accelerate timelines, focusing on therapeutic areas including cancer, neurological, and autoimmune diseases.

The recent $200 million Series A extension was led by Fidelity Management & Research Company, with participation from RiverVest Venture, Lightchain Capital, Abingworth, ICG, LYZZ Capital, Tybourne Capital, Aisling Capital, and others. This funding will support the advancement of Treeline’s pipeline, which includes small molecules, degraders and glues, and targeted therapy antibody-drug conjugates (TT-ADCs). The company plans to submit an investigational new drug (IND) application for a fourth program early next year and has three other internal programs set to enter IND-enabling studies after the Phase 1 readouts.

Treeline’s investor syndicate includes several prominent firms, such as 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.

The company’s approach to drug discovery emphasizes a data-driven strategy, aiming to create precision medicines that address the underlying causes of diseases. By leveraging both established and emerging technologies, including biology, chemistry, structural biology, and computation, Treeline seeks to build therapies that prioritize molecular targets in oncology that are validated but difficult to drug.

With the initiation of these clinical trials and the substantial funding secured, Treeline Biosciences is poised to advance its mission of developing innovative treatments for cancer and other serious diseases. The company’s progress will be closely watched by the biotech community and investors alike as it moves forward with its clinical programs.

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