Tirabrutinib

DB15227InvestigationalSmall molecule

Tirabrutinib is under investigation in clinical trial NCT02626026 (Safety and Pharmacokinetics of GS-4059 in Healthy Volunteers and Subjects With Rheumatoid Arthritis (RA)).

Mechanism: Pharmacologically active on Tyrosine-protein kinase BTK
Curator reviewed
Formula / weight: C₂₅H₂₂N₆O₃ · 454.49 g/mol (avg)
Also known as: ONO-4059 (free base)
Code names: GS-4059 · ONO-4059

Resolves to

Compound

UNIILXG44NDL2TCAS1351636-18-4ChEMBLCHEMBL4071161

Clinical / RWD

ATCL01EL06

Structure

InChIKeySEJLPXCPMNSRAM-GOSISDBHSA-NSMILESCC#CC(=O)N1CC[C@H](C1)N1C(=O)N(C2=C(N)N=CN=C12)C1=CC=C(OC2=CC=CC=C2)C=C1

Targets

Q06187BTK

What you can answer from here — as of July 17, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

13Clinical trialsPhase, status and sponsor resolved per trial

1ATC codeIncluding every combination product, plus 4 drug categories

5+ReferencesStructured and connected to the statements they support

Which drugs share a target with Tirabrutinib, and which of those have an active Phase 3 trial?

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