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Clinical Trials Exploring BTK


An investigational, selective non-covalent Bruton's tyrosine kinase (BTK) inhibitor with preclinical potency against both wild-type and cysteine-481–mutated BTK (C481S) and improved selectivity compared with other BTK inhibitors.

Exploring BTK

For more information, call 1-855-LOXO-305 or email

NCT03740529 open_in_new

A Phase 1/2 Study of Oral LOXO-305 in Patients With Previously Treated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) or B-cell non-Hodgkin’s Lymphoma (NHL)

This is a phase 1/2, open-label, first-in-human study designed to evaluate the safety, tolerability, pharmacokinetics, and overall response rate of LOXO-305 in patients with previously treated CLL/SLL, Waldenström’s macroglobulinemia (WM)/mantle cell lymphoma (MCL)/marginal zone lymphoma (MZL), follicular lymphoma, diffuse large B-cell lymphoma, or other B-cell NHL who have failed or are intolerant to the standard of care.

See Trial Information and Study Locations

About BTK

BTK, one of the 5 members of the Tec family of non-receptor tyrosine kinases, plays a critical role in oncogenic signaling.1 BTK is a cytoplasmic tyrosine kinase, and its activation results in downstream signaling that controls nuclear factor-κB, which is essential for normal B-cell function.1,2 BTK plays a critical role in the proliferation and survival of leukemic B-cells and is implicated in various B-cell malignancies including CLL, MZL, MCL, and WM.1,3

For additional information about the LOXO-305 clinical trial, please refer to

Interested physicians and patients may contact us at +1-855-LOXO-305 or email

Policy for Access to Investigational Agents

Loxo Oncology is committed to helping patients who have not responded to available therapies and may benefit from its investigational therapies. Loxo Oncology's Policy for Access to Investigational Agents describes the principles and government regulations that the company will follow when considering a request.

  1. Pal Singh S, Dammeijer F, Hendriks RW. Role of Bruton’s tyrosine kinase in B cells and malignancies. Mol Cancer. 2018; 17:57-018-0779-z
  2. Bajpai UD, Zhang K, Teutsch M, et al. Bruton's tyrosine kinase links the B cell receptor to nuclear factor κB activation. J Exp Med. 2000;191(10):1735-1744.
  3. Cinar M, Hamdani F, Mo Z, et al. Bruton tyrosine kinase is commonly overexpressed in mantle cell lymphoma and its attenuation by Ibrutinib induces apoptosis. Leuk Res. 2013;37(10):1271-1277.

For more information, call +1-855-LOXO-305
or email