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
| 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 |
| Comparator or background therapy1 trial | ||||||
| — | NCT04087876 Background | — | intrahepatic cholangiocarcinoma | Basilea Pharmaceutica | No longer available | No outcome recorded |
News releases announcing trial results or a regulatory action · 17
| Date | Issuer | Release |
|---|---|---|
| 2022-04-13 | Basilea Pharmaceutica | Results Basilea reports preclinical data on oncology drug candidates BAL0891, derazantinib and lisavanbulin at AACR Annual Meeting basilea.com ↗
Derazantinib, an FGFR1-3 inhibitor, inhibits CSF1R in macrophages and tumor cell lines and synergizes with a PDL1-antibody in an FGFR-driven murine syngeneic model |
| 2022-01-24 | Basilea Pharmaceutica | Results Basilea reports updated interim results for iCCA patients with FGFR2 mutations and amplifications from phase 2 study FIDES-01 at ASCO GI Cancers Symposium basilea.com ↗
Based on investigator assessments, the disease control rate (DCR) was 74%, including two patients with a confirmed objective response and 15 patients with stable disease, where tumor shrinkage was observed in the majority of patients. |
| 2021-10-11 | Basilea Pharmaceutica | Results Basilea presents preclinical data on synergy between derazantinib and paclitaxel in gastric tumor models at ANE Conference basilea.com ↗
In the preclinical studies, synergistic anti-tumor effects were reported across a number of gastric cancer models, including in-vivo tumor models with different FGFR aberrations. |
| 2021-09-17 | Basilea Pharmaceutica | Results Basilea presents full safety and efficacy data set on derazantinib in patients with FGFR2 fusion-positive iCCA at ESMO congress basilea.com ↗
Importantly, the progression-free survival (PFS) further increased to 8.0 months (previously: 7.8 months). |
| 2021-05-31 | Basilea Pharmaceutica | Results Basilea provides updates on efficacy data with derazantinib in bile duct cancer and on ongoing clinical programs in urothelial and gastric cancer basilea.com ↗
An updated analysis shows further improvement of progression-free survival, disease control rate and objective response rate in the cohort of FGFR2 gene fusion-positive patients with bile duct cancer (iCCA) in FIDES-01 study |
| 2021-03-24 | Basilea Pharmaceutica | Results Basilea reports positive interim results from phase 2 study FIDES-01 for derazantinib in FGFR2 gene mutation- or amplification-positive patients with bile duct cancer (iCCA) basilea.com ↗
The pre-specified criterion that at least 8 patients met the primary endpoint of obtaining progression-free survival (PFS) of at least 3 months was successfully achieved. |
| 2021-02-12 | Basilea Pharmaceutica | Results Basilea reports derazantinib/PD-L1 checkpoint inhibitor combination results from dose-finding part of FIDES-02 study in patients with solid tumors at ASCO GU symposium basilea.com ↗
The derazantinib-atezolizumab combination was well tolerated and no dose-limiting toxicities were observed. |
| 2021-02-10 | Basilea Pharmaceutica | Results Basilea reports positive topline results from phase 2 study FIDES-01 for derazantinib in FGFR2 gene fusion-positive patients with bile duct cancer (iCCA) basilea.com ↗
The objective response rate (ORR) is 20.4% based on 21 patients with a confirmed partial response. |
| 2020-10-26 | Basilea Pharmaceutica | Results Basilea presents preclinical data on anti-angiogenic activity of derazantinib at ENA 2020 basilea.com ↗
The presented data from several preclinical models demonstrate that derazantinib has an anti-angiogenic effect, which may contribute to its overall anti-tumor activity in FGFR-driven cancers. |
| 2020-10-13 | Basilea Pharmaceutica | Results Basilea reports interim results from phase 1/2 study FIDES-02 exploring derazantinib in patients with advanced urothelial cancer basilea.com ↗
The Recommended Phase 2 Dose (RP2D) for the combination has been determined and phase 2 expansion substudies are now open for enrolment. |
| 2020-10-12 | Basilea Pharmaceutica | Results Basilea reports pooled efficacy data for derazantinib in iCCA patients with FGFR2 gene mutations and amplifications presented at ESMO MAP Virtual Congress 2020 basilea.com ↗
The median progression free survival was 7.2 months and patients received treatment for a median of 8.2 months. |
| 2020-07-28 | Basilea Pharmaceutica | Results Basilea announces data presentations at ESMO Virtual Congress 2020 basilea.com ↗
Furthermore, derazantinib shows promising efficacy in patient-derived tumor models with gene aberrations in FGFR1-3. |
| 2020-01-23 | Basilea Pharmaceutica | Results Basilea reports activity of derazantinib in preclinical models of gastric cancer at ASCO Gastrointestinal Cancers Symposium basilea.com ↗
Basilea Pharmaceutica Ltd. (SIX: BSLN) reported today that its oncology drug candidate derazantinib showed convincing activity in preclinical models of gastric cancer with FGFR genetic aberrations. |
| 2019-10-30 | Basilea Pharmaceutica | Results Basilea reports positive preclinical data on oncology drug candidates derazantinib and lisavanbulin at AACR-NCI-EORTC conference basilea.com ↗
In a late-breaking abstract, novel preclinical data were presented demonstrating that derazantinib has equipotent inhibitory activity against fibroblast growth factor receptor kinases (FGFR1, 2 and 3) and the colony-stimulating factor 1 receptor (CSF1R) kinase. |
| 2019-09-30 | Basilea Pharmaceutica | Results Basilea reports at ESMO meeting that drug candidate derazantinib showed clinical benefit in intrahepatic cholangiocarcinoma (iCCA) patients with various FGFR2 genetic aberrations basilea.com ↗
The analysis shows that derazantinib provided clinically meaningful anti-tumor activity, not only in iCCA patients with FGFR2 gene fusions, but also in iCCA patients with FGFR2 gene mutations and amplifications. |
| 2019-06-03 | Basilea Pharmaceutica | Results Basilea reports publication of clinical data for anticancer drug candidates BAL101553 in glioblastoma and derazantinib in intrahepatic cholangiocarcinoma at ASCO meeting basilea.com ↗
For derazantinib, Basilea's most advanced oncology drug candidate, data from a post-hoc analysis from a previously completed non-comparative phase 2a study7 were published in abstract form. |
| 2019-01-09 | Basilea Pharmaceutica | Results Basilea reports positive interim results from registrational phase 2 study with oncology drug candidate derazantinib in intrahepatic cholangiocarcinoma (iCCA) basilea.com ↗
The objective response rate (ORR) in these 29 patients was 21%. |
All press releases naming this drug 25 releases
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 NCT04098692 ↗ |
| 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 |