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WNT974 · 1 trial · 1 indication
Phase Ib: To estimate the MTD(s) and/or RP2D(s) of the triple combination of WNT974, LGX818 and cetuximab in patients with BRAFV600-mutant, KRAS wild-type (WT) mCRC harboring upstream Wnt pathway mutations.
Phase II: To estimate the preliminary anti-tumor activity of the RP2D(s) of the combination of WNT974, LGX818 and cetuximab in patients with BRAFV600-mutant metastatic CRC harboring upstream Wnt pathway mutations
| Arm | Type | Description |
|---|---|---|
| WNT974, LGX818 and cetuximab combo | EXPERIMENTAL | Phase l: Dose Escalation phase; Phase ll: SIngle group assessing the triple combination of WNT974, LGX818 and cetuximab |
| Name | Type | Description |
|---|---|---|
| WNT974 | DRUG | - |
| LGX818 | DRUG | - |
| Cetuximab | BIOLOGICAL | - |
Inclusion Criteria: * Male or female aged ≥ 18 years * Histological or cytological confirmed metastatic colorectal cancer * Written documentation of KRAS wild-type status and BRAFV600-mutation with RNF43 mutation and/or RSPO fusion * Progression of disease after at least one prior standard of care ...
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WNT974 is an investigational small molecule being studied for the treatment of metastatic colorectal cancer, specifically in patients whose tumors carry BRAF mutations and Wnt pathway mutations. It is a Phase 1 agent and has not been approved for any indication.
WNT974 targets PORCN, a membrane-bound O-acyltransferase enzyme. By inhibiting PORCN, WNT974 blocks Wnt ligand secretion and downstream Wnt pathway signaling, which is a mechanism of interest in cancers driven by aberrant Wnt activation such as metastatic colorectal cancer.
WNT974 is being developed by Pfizer, Inc., which trades on the New York Stock Exchange under the ticker PFE. Pfizer is the sponsor of the clinical program evaluating this agent in metastatic colorectal cancer.
WNT974 is in Phase 1 clinical development. It is an investigational agent and has not received FDA approval. The Phase 1 program has completed, with one completed trial and no active trials currently listed.
WNT974 has been evaluated in one completed Phase 1 trial, NCT02278133, titled Study of WNT974 in Combination With LGX818 and Cetuximab in Patients With BRAF-mutant Metastatic Colorectal Cancer (mCRC) and Wnt Pathway Mutations. The trial enrolled 20 patients across the United States, Australia, Belgium, Canada, France, Israel, Italy, Netherlands, Singapore, and Spain.