Drugs / Derazantinib
Derazantinib
also known as
AQ14741087 · ARQ 087 · ARQ 087.2HCl · ARQ-087 DIHYDROCHLORIDE · Derazantinib dihydrochloride · DERAZANTINIB HYDROCHLORIDE
Small molecule targets FGFR1, FGFR2 via inhibition
Trials 6 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 11 trial | ||||||
| Phase 1 | NCT04098692 | Aug → Nov 2019 | — | Basilea Pharmaceutica | Completed | No outcome recorded |
| Phase 1/23 trials | ||||||
| Phase 1/2 | NCT04604132 | Oct 2020 → Nov 2022 | gastric adenocarcinoma | Basilea Pharmaceutica | Terminated | No outcome recorded |
| Phase 1/2 | NCT04045613 | Aug 2019 → Oct 2022 | urothelial carcinoma | Basilea Pharmaceutica | Completed | No outcome recorded |
| Phase 1/2 | NCT01752920 | Dec 2012 → Aug 2018 | neoplasm | Basilea Pharmaceutica | Completed | No outcome recorded |
| Phase 22 trials | ||||||
| Phase 2 | NCT05174650 | Apr 2022 → Dec 2025 overdue | intrahepatic cholangiocarcinoma | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Active not recruiting | No outcome recorded |
| Phase 2 | NCT03230318 | Sep 2017 → Oct 2022 | combined hepatocellular carcinoma and cholangiocarcinoma, intrahepatic cholangiocarcinoma | Basilea Pharmaceutica | Completed | No outcome recorded |
Also used as a comparator or background therapy in 1 trial
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| — | NCT04087876 Background | — | intrahepatic cholangiocarcinoma | Basilea Pharmaceutica | No longer available | No outcome recorded |
Evidence & citations 12 cited values
Every value below carries the sentence it was read from. 10 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Derazantinib | ClinicalTrials.gov intervention name — accepted as the source's own label NCT05174650 ↗ |
| Known as | AQ14741087 | ChEMBL registry synonym — accepted as the source's own label CHEMBL4297187 ↗ |
| Known as | ARQ 087 | “Derazantinib (ARQ 087), an orally bioavailable, multi-kinase inhibitor with potent pan-FGFR activity, has shown preliminary therapeutic activity against FGFR2 fusion-positive iCCA.” PMID 30420614 ↗ Nov 2018 |
| Known as | ARQ 087.2HCl | ChEMBL registry synonym — accepted as the source's own label CHEMBL4297187 ↗ |
| Known as | ARQ-087 DIHYDROCHLORIDE | ChEMBL registry synonym — accepted as the source's own label CHEMBL4297187 ↗ |
| Known as | Derazantinib dihydrochloride | ChEMBL registry synonym — accepted as the source's own label CHEMBL4297187 ↗ |
| Known as | DERAZANTINIB HYDROCHLORIDE | ChEMBL registry synonym — accepted as the source's own label CHEMBL4297187 ↗ |
| Action | Inhibit | “inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) was evident by the response to ARQ 087 treatment.” PMID 27627808 ↗ Sep 2016 |
| Modality | Small molecule | “ARQ 087 is a novel, ATP competitive, small molecule, multi-kinase inhibitor with potent in vitro and in vivo activity against FGFR addicted cell lines and tumors.” PMID 27627808 ↗ Sep 2016 |
| Route | Oral | “Derazantinib was administered orally” NCT01752920 ↗ |
| Target | FGFR1 | “Biochemically, ARQ 087 exhibited IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3.” PMID 27627808 ↗ Sep 2016 |
| Target | FGFR2 | “Biochemically, ARQ 087 exhibited IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3.” PMID 27627808 ↗ Sep 2016 |