roblitinib

selective, reversible covalent inhibitor of FGFR4

Also Known As:

7-formyl-6-(4-methyl-2-oxo-piperazin-1-ylmethyl)-3,4-dihydro-2H-(1,8)naphthyridine-1-carboxylic acid (5-cyano-4-(2-methoxy-ethylamino)-pyridin-2-yl)-amide; FGF401; N-(5-cyano-4-(2-methoxyethylamino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide

Networked: 9 relevant articles (0 outcomes, 6 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - roblitinib: 9
  - Piperazines: 26
    - roblitinib: 9

Experts

1.	Gu, Yi: 2 articles (06/2022 - 01/2022)
2.	Katsanou, Vasiliki: 2 articles (06/2022 - 01/2022)
3.	Myers, Andrea: 2 articles (06/2022 - 01/2022)
4.	Porta, Diana Graus: 2 articles (06/2022 - 11/2020)
5.	Huynh, Hung: 2 articles (10/2021 - 11/2020)
6.	Le, Thi Bich Uyen: 2 articles (10/2021 - 11/2020)
7.	Prawira, Aldo: 2 articles (10/2021 - 11/2020)
8.	Wang, Youzhen: 2 articles (11/2020 - 12/2019)
9.	Couttet, Philippe: 2 articles (12/2019 - 01/2018)
10.	Fairhurst, Robin A: 2 articles (12/2019 - 01/2018)

Related Diseases

1.	Neoplasms (Cancer) 12/01/2019 - "FGF401 is the first FGFR4 inhibitor to enter clinical trials, and a phase I/II study is currently ongoing in HCC and other solid malignancies." 12/01/2019 - "FGF401 has remarkable antitumor activity in mice bearing HCC tumor xenografts and patient-derived xenograft models that are positive for FGF19, FGFR4, and KLB. " 04/22/2023 - "Moreover, the HCC cell lines, zebrafish/mouse HCC xenografts and zebrafish HCC primary tumors were treated with FGFR4 inhibitor (Roblitinib) and/or EZH2 inhibitor (CPI-169) and then subjected to cell proliferation, viability, apoptosis, and tumor growth analyses to evaluate the feasibility of combination therapy for HCC both in vitro and in vivo. " 11/01/2020 - "Furthermore, FGF401 inhibited the FGF19/FGFR-4 signaling pathway, cell proliferation, and hypoxia, induced apoptosis and blood vessel normalization and prolonged the overall survival (OS) of mice bearing high FGF19 tumors. " 10/01/2021 - "Our findings suggest that HCC patients with high FGFR2/3 or FGF19/FGFR4 expressing tumors might benefit from a combination infigratinib/FGF401; thus, supporting its evaluation in clinical trials."
2.	Hepatocellular Carcinoma (Hepatoma) 01/01/2018 - "FGF401 is a highly selective FGFR4 kinase inhibitor being developed for hepatocellular carcinoma, currently in phase I/II clinical studies. " 11/01/2020 - "FGF401 and vinorelbine synergistically mediate antitumor activity and vascular normalization in FGF19-dependent hepatocellular carcinoma." 06/02/2022 - "A first-in-human phase 1/2 study of FGF401 and combination of FGF401 with spartalizumab in patients with hepatocellular carcinoma or biomarker-selected solid tumors." 01/01/2022 - "Contribution of machine learning to tumor growth inhibition modeling for hepatocellular carcinoma patients under Roblitinib (FGF401) drug treatment." 01/01/2022 - "Data from 127 patients with hepatocellular carcinoma enrolled in a phase I/II study evaluating once-daily oral doses of the fibroblast growth factor receptor FGFR4 kinase inhibitor, Roblitinib (FGF401), were used. "
3.	Diarrhea 12/01/2022 - "Exposure-safety analyses on the expected on-target adverse events, including elevation of aspartate aminotransferase and diarrhea, indicated a lack of clinically relevant relationship with FGF401 exposure. " 01/01/2018 - "In preclinical studies in mice and dogs, oral administration of FGF401 led to induction of Cyp7a1, elevation of its peripheral marker 7alpha-hydroxy-4-cholesten-3-one, increased BA pool size, decreased serum cholesterol and diarrhea in dogs. "
4.	Liver Neoplasms (Liver Cancer) 12/01/2019 - "FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer."
5.	Hypoxia (Hypoxemia) 11/01/2020 - "Furthermore, FGF401 inhibited the FGF19/FGFR-4 signaling pathway, cell proliferation, and hypoxia, induced apoptosis and blood vessel normalization and prolonged the overall survival (OS) of mice bearing high FGF19 tumors. "

Related Drugs and Biologics

1.	Phosphotransferases (Kinase)
2.	roblitinib
3.	Biomarkers (Surrogate Marker)
4.	Fibroblast Growth Factor Receptors (Fibroblast Growth Factor Receptor)
5.	Cholesterol
6.	Vinorelbine (Navelbine)
7.	infigratinib
8.	7 alpha-hydroxy-4-cholesten-3-one
9.	spartalizumab
10.	Type 4 Fibroblast Growth Factor Receptor

Related Therapies and Procedures

1.	Oral Administration
2.	Therapeutics