Therapy Detail
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| Therapy Name | Derazantinib |
| Synonyms | |
| Therapy Description |
Derazantinib (ARQ 087) is an ATP-competitive multi-kinase inhibitor with activity against Fgfr 1/2, FGFR fusions, Arg, Lck, and Kit, which prevents cell proliferation and angiogenesis (PMID: 27627808). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Derazantinib | ARQ 087 | FGFR1 Inhibitor 27 FGFR2 Inhibitor 22 KIT Inhibitor 56 LCK Inhibitor 6 | Derazantinib (ARQ 087) is an ATP-competitive multi-kinase inhibitor with activity against Fgfr 1/2, FGFR fusions, Arg, Lck, and Kit, which prevents cell proliferation and angiogenesis (PMID: 27627808). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR1 fusion | hematologic cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of hematologic cancer cells harboring FGFROP2-FGFR1 fusion in culture (PMID: 27627808). | 27627808 |
| KIT over exp | Advanced Solid Tumor | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Kit in culture (PMID: 27627808). | 27627808 |
| FGFR2 fusion | intrahepatic cholangiocarcinoma | sensitive | Derazantinib | Phase II | Actionable | In a Phase II trial (FIDES-01), Derazantinib (ARQ 087) treatment resulted in an objective response rate of 21.4%, a disease control rate of 75.7%, median progression-free survival of 8.0 months, and a median overall survival of 17.2 months in patients with intrahepatic cholangiocarcinoma harboring an FGFR2 fusion (Ann Oncol (2022) 33 (suppl_7): S19-S26; NCT03230318). | detail... |
| FGFR2 fusion | intrahepatic cholangiocarcinoma | sensitive | Derazantinib | Phase I | Actionable | In a Phase Ib/II trial, Derazantinib (ARQ 087) treatment resulted in an overall response rate of 20.7% (6/29), a disease control rate of 82.8% (24/29), and a median progression-free survival of 5.7 months in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (PMID: 30420614; NCT01752920). | 30420614 |
| FGFR1 over exp | Advanced Solid Tumor | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr1 in culture (PMID: 27627808). | 27627808 |
| FGFR2 amp | breast cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of breast cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). | 27627808 |
| FGFR2 N549K | endometrial cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cell lines harboring FGFR2 N549K in culture (PMID: 27627808). | 27627808 |
| FGFR2 amp | intrahepatic cholangiocarcinoma | predicted - sensitive | Derazantinib | Phase II | Actionable | In a Phase II trial (FIDES-01), Derazantinib (ARQ 087) treatment resulted in an objective response rate of 6.5%, a disease control rate of 58.1%, median progression-free survival of 8.3 months, and a median overall survival of 15.9 months in patients with intrahepatic cholangiocarcinoma harboring an FGFR2 mutation or amplification (Ann Oncol (2022) 33 (suppl_7): S19-S26; NCT03230318). | detail... |
| FGFR3 K652E | urinary bladder cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3 K652E in culture (PMID: 27627808). | 27627808 |
| FGFR2 over exp | Advanced Solid Tumor | sensitive | Derazantinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr2 in culture and in cell line xenograft models (PMID: 27627808). | 27627808 |
| FGFR2 fusion FGFR2 amp | stomach cancer | sensitive | Derazantinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification and PDHX-FGFR2 fusion in culture, resulted in tumor regression in cell line xenograft models (PMID: 27627808). | 27627808 |
| FGFR2 mutant | intrahepatic cholangiocarcinoma | predicted - sensitive | Derazantinib | Phase II | Actionable | In a Phase II trial (FIDES-01), Derazantinib (ARQ 087) treatment resulted in an objective response rate of 6.5%, a disease control rate of 58.1%, median progression-free survival of 8.3 months, and a median overall survival of 15.9 months in patients with intrahepatic cholangiocarcinoma harboring an FGFR2 mutation or amplification (Ann Oncol (2022) 33 (suppl_7): S19-S26; NCT03230318). | detail... |
| FGFR1 amp | adrenocortical carcinoma | sensitive | Derazantinib | Phase I | Actionable | In a Phase I trial, ARQ 087 treatment resulted in stable disease with a tumor reduction of 20% in an adrenocortical carcinoma patient harboring FGFR1 amplification, who remained on study for 3.5 years (PMID: 28972963; NCT01752920). | 28972963 |
| FGFR2 amp | stomach cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). | 27627808 |
| FGFR2 S252W | endometrial cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 27627808). | 27627808 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03230318 | Phase II | Derazantinib | Derazantinib in Subjects With FGFR2 Gene Fusion-, Mutation- or Amplification- Positive Inoperable or Advanced Intrahepatic Cholangiocarcinoma (FIDES-01) | Completed | USA | ITA | FRA | ESP | DEU | CAN | BEL | 4 |
| NCT04604132 | Phase Ib/II | Atezolizumab + Derazantinib Derazantinib + Paclitaxel + Ramucirumab Derazantinib Paclitaxel + Ramucirumab | Derazantinib Alone or in Combination With Paclitaxel, Ramucirumab or Atezolizumab in Gastric Adenocarcinoma (FIDES-03) | Terminated | USA | ITA | FRA | ESP | DEU | BEL | 9 |
| NCT04045613 | Phase Ib/II | Derazantinib Atezolizumab + Derazantinib | Derazantinib and Atezolizumab in Patients With Urothelial Cancer (FIDES-02) | Completed | USA | ITA | FRA | ESP | DEU | CAN | AUT | 7 |
| NCT01752920 | Phase I | Derazantinib | Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors | Completed | USA | ITA | 0 |
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