Drug intelligence / Profile preview

imatinib + acetaminophen

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of imatinib and acetaminophen**, used together rather than as a single fixed-dose formulation. **Imatinib** is an oral small molecule tyrosine kinase inhibitor primarily targeting BCR-ABL, c-KIT, and PDGFR kinases, and is used to treat **chronic myelogenous leukemia (CML)**, gastrointestinal stromal tumors (GIST), and some other cancers. **Acetaminophen** (paracetamol) is a widely used small molecule analgesic and antipyretic. When combined, there are significant pharmacokinetic drug–drug interactions: imatinib increases acetaminophen plasma levels due to inhibition of acetaminophen glucuronidation. Experimental and clinical data suggest that chronic acetaminophen therapy should be avoided in patients on imatinib because of increased toxicity risk, though limited human data show single-dose co-administration may not require dose adjustment and is generally tolerated[2][4][5][1].

Brand names
Gleevec + TylenolGlivec + Tylenol (and all generic combinations)
Other names
imatinib mesylate + paracetamol
02

Targets

ABL1 myristoyl pocketKIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)COX

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