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loxo-305

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Overview

NCI Definition [1]:
An orally available, selective, non-covalent Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Upon oral administration, BTK inhibitor LOXO-305 selectively and reversibly binds to BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, thereby inhibiting the growth of malignant B-cells that overexpress BTK. Reversible binding of LOXO-305 may preserve antitumor activity in the presence of certain acquired resistance mutations, including C481 mutated BTK, and limit toxicity associated with inhibition of other non-BTK kinases. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed or mutated in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B-lymphocytes.

Clinical Trials

View Clinical Trials for loxo-305

Loxo-305 has been investigated in 3 clinical trials, of which 3 are open and 0 are closed. Of the trials investigating loxo-305, 1 is phase 1/phase 2 (1 open) and 2 are phase 3 (2 open).

Chronic lymphocytic leukemia/small lymphocytic lymphoma, mantle cell lymphoma, and blastoid variant mantle cell lymphoma are the most common diseases being investigated in loxo-305 clinical trials [2].

Drug Details

Synonyms [2]:
btk inhibitor loxo-305, loxo305, loxo 305, pirtobrutinib, 5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-((2s)-1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide, ly3527727
Drug Target(s) [2]:
BTK
NCIT ID [1]:
C158617

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.