Drug intelligence / Profile preview

TAS5315 + methotrexate

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

**TAS5315 + methotrexate** is a combination of TAS5315, a highly selective, irreversible covalent small molecule inhibitor of Bruton’s tyrosine kinase (BTK), and methotrexate, a small molecule antimetabolite and folate pathway inhibitor. This combination has been studied primarily for the treatment of **rheumatoid arthritis (RA)**, particularly in patients who are refractory or have inadequate response to methotrexate monotherapy[3][7]. - **TAS5315** acts by inhibiting BTK, thereby modulating B-cell receptor signaling, reducing immune cell activation, and inflammation[1][3][5][7][9]. - **Methotrexate** inhibits dihydrofolate reductase and other enzymes in the folate pathway, impairing nucleotide synthesis and suppressing inflammation as a disease-modifying antirheumatic drug (DMARD)[2][4][6][8][10]. This combination aims to achieve greater efficacy in controlling disease activity in RA by targeting both B-cell signaling and systemic inflammation pathways.

Other names
MethotrexateMTX
02

Targets

BLK (B lymphoid tyrosine kinase)JAK3 (Janus kinase 3)ERBB4 (Erb-b2 receptor tyrosine kinase 4)DHFR (Dihydrofolate reductase)EGFR T790M (Epidermal growth factor receptor T790M mutant)TXKITK (Interleukin 2-inducible T-cell kinase)BTK (Bruton tyrosine kinase)

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