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momelotinib + nab-paclitaxel + gemcitabine
- Development stage
- Unknown
- Lead developer
- Gilead Sciences
- Modality
- Recombinant Proteins and Enzymes, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination drug regimen consisting of momelotinib, nab-paclitaxel (albumin-bound paclitaxel), and gemcitabine. Momelotinib is an orally administered, ATP-competitive small molecule inhibitor of Janus kinase 1 (JAK1), Janus kinase 2 (JAK2), and Activin A receptor type I (ACVR1), as well as several other kinases including TANK-binding kinase 1 (TBK1). It was evaluated in combination with nab-paclitaxel and gemcitabine, both of which are antineoplastic agents, in clinical trials for previously untreated metastatic pancreatic ductal adenocarcinoma. The therapeutic rationale was to combine targeted inhibition of JAK/STAT signaling and hepcidin regulation (by momelotinib) with cytotoxic chemotherapy. Phase 1 and 3 clinical trials showed that while the regimen was generally safe and tolerable, no significant improvement in clinical efficacy over nab-paclitaxel and gemcitabine alone was demonstrated in pancreatic cancer. The regimen has not received marketing approval for this indication.
- Other names
- momelotinib + nab-paclitaxel + gemcitabine
02
Targets
TUBB (Tubulin (alpha and beta subunits))JAK2 (Janus kinase 2)TBK1 (TANK binding kinase 1)JAK1 (Janus kinase 1)RNR (Ribonucleotide reductase)ACVR1 (Activin receptor type I)DNA polymerase family
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