Drug intelligence / Profile preview

orelabrutinib + methotrexate

Development stage
Unknown
Lead developer
Innocare
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Orelabrutinib + methotrexate is an investigational combination regimen that pairs orelabrutinib, an oral, highly selective, second-generation Bruton's tyrosine kinase (BTK) inhibitor, with methotrexate, a folate analog metabolic inhibitor and cytotoxic chemotherapy (typically administered at high doses, HD-MTX). Orelabrutinib is designed to cross the blood-brain barrier and achieve high concentrations in the cerebrospinal fluid (CSF), making this combination particularly suitable for treating central nervous system (CNS) malignancies. The regimen is primarily being evaluated, often in combination with rituximab (forming the ORM or R-MO regimen), as an induction therapy for newly diagnosed or relapsed/refractory primary central nervous system lymphoma (PCNSL) and other B-cell malignancies of the CNS.

Other names
methotrexate + orelabrutinibmethotrexate and orelabrutinibmethotrexate plus orelabrutiniborelabrutinib and methotrexateorelabrutinib plus methotrexate
02

Targets

DHFR (Dihydrofolate reductase)BTK (Bruton tyrosine kinase)

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