Drug intelligence / Profile preview

ruxolitinib + capecitabine + regorafenib

Development stage
Phase 2
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination regimen of three oral small molecule drugs: **ruxolitinib, capecitabine, and regorafenib**. - **Ruxolitinib** is a selective inhibitor of Janus kinase 1 (JAK1) and Janus kinase 2 (JAK2), originally developed for myeloproliferative neoplasms. It acts by inhibiting the JAK-STAT pathway, reducing inflammatory cytokine signaling which can modulate the tumor microenvironment[1][4][5]. - **Capecitabine** is an oral prodrug of 5-fluorouracil (5-FU), a pyrimidine antimetabolite that inhibits DNA synthesis by blocking thymidylate synthase, leading to cell death in rapidly dividing tumor cells[2][7]. - **Regorafenib** is an oral multi-kinase inhibitor that targets multiple protein kinases involved in tumor angiogenesis (e.g. VEGFR1–3, TIE2), oncogenesis (e.g. KIT, RET, BRAF), and modulation of the tumor microenvironment (e.g. PDGFR, FGFR)[1][3][4][6][7]. This triple drug regimen is not an approved fixed-dose combination but has been investigated (in subgroups or parallel studies) for **advanced/metastatic colorectal cancer** and **metastatic pancreatic cancer** resistant to prior treatments. The rationale behind combining these drugs is to target multiple relevant pathways in tumor biology (inflammation, DNA synthesis, angiogenesis) in highly refractory malignancies[1][2][4][5][7].

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)PDGFRA (Platelet-derived growth factor receptor alpha)TYMP (Thymidine phosphorylase)

Beyond the preview

Go deeper on ruxolitinib + capecitabine + regorafenib.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on ruxolitinib + capecitabine + regorafenib.

Gosset Free

Get started with Gosset.

Enter your corporate email.

Work email preferred.

Book a call