derazantinib (ARQ 087) / Merck (MSD) 
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 1 Disease   4 Trials   4 Trials   159 News 


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  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD)
    Journal:  Derazantinib Inhibits the Bioactivity of Keloid Fibroblasts via FGFR Signaling. (Pubmed Central) -  Dec 23, 2023   
    Also, derazantinib inhibited the expression of FGFR1 and PAI-1 and reduced the weight of the implanted keloid from the xenograft mice model. These findings suggest that derazantinib may be a potent therapy for keloids via FGFR signaling.
  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD)
    PK/PD data, Preclinical, Journal:  Lack of pharmacokinetic interaction between derazantinib and naringin in rats. (Pubmed Central) -  Mar 14, 2023   
    Co-administration of naringin with derazantinib was not associated with significant changes in pharmacokinetic parameters. Thus, this study suggests that the combination of derazantinib with naringin can safely be administered concomitantly without dose adjustment.
  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD), paclitaxel / Generic mfg.
    Preclinical, Journal:  The fibroblast growth factor receptor inhibitor, derazantinib, has strong efficacy in human gastric tumor models and synergizes with paclitaxel in vivo. (Pubmed Central) -  Mar 13, 2023   
    The combination showed synergy (5) or additivity (2), and no antagonism, with synergy significantly associated (P < 0.05) with higher levels of M2-type macrophages. The association of strong efficacy of the combination in vivo with M2 macrophages, which are known to express CSF1R, and the absence of synergy in vitro is consistent with the tumor microenvironment also being a factor in DZB efficacy and suggests additional means by which DZB could be stratified for cancer treatment in the clinic.
  • ||||||||||  Cyramza (ramucirumab) / Eli Lilly, derazantinib (ARQ 087) / Merck (MSD), Tecentriq (atezolizumab) / Roche
    Trial termination, Combination therapy, Monotherapy:  FIDES-03: Derazantinib Alone or in Combination With Paclitaxel, Ramucirumab or Atezolizumab in Gastric Adenocarcinoma (clinicaltrials.gov) -  Feb 16, 2023   
    P1b/2,  N=47, Terminated, 
    The association of strong efficacy of the combination in vivo with M2 macrophages, which are known to express CSF1R, and the absence of synergy in vitro is consistent with the tumor microenvironment also being a factor in DZB efficacy and suggests additional means by which DZB could be stratified for cancer treatment in the clinic. Completed --> Terminated; Terminated prematurely for administrative reasons not related to patient safety.
  • ||||||||||  Cyramza (ramucirumab) / Eli Lilly, derazantinib (ARQ 087) / Merck (MSD), Tecentriq (atezolizumab) / Roche
    Trial completion, Trial completion date, Trial primary completion date, Combination therapy, Monotherapy:  FIDES-03: Derazantinib Alone or in Combination With Paclitaxel, Ramucirumab or Atezolizumab in Gastric Adenocarcinoma (clinicaltrials.gov) -  Jan 17, 2023   
    P1b/2,  N=47, Completed, 
    These data confirm CSF1R as an important oncology target for DZB and provide mechanistic insight for the ongoing clinical trials, in which DZB is combined with the PD-L1 antibody, atezolizumab. Active, not recruiting --> Completed | Trial completion date: Jul 2023 --> Dec 2022 | Trial primary completion date: Jul 2023 --> Dec 2022
  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD), Tecentriq (atezolizumab) / Roche
    Trial completion, Trial completion date, Trial primary completion date:  FIDES-02: Derazantinib and Atezolizumab in Patients With Urothelial Cancer (clinicaltrials.gov) -  Oct 20, 2022   
    P1b/2,  N=95, Completed, 
    Active, not recruiting --> Completed Active, not recruiting --> Completed | Trial completion date: Oct 2023 --> Sep 2022 | Trial primary completion date: Jul 2023 --> Sep 2022
  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD), Tecentriq (atezolizumab) / Roche
    Enrollment closed, Enrollment change:  FIDES-02: Derazantinib and Atezolizumab in Patients With Urothelial Cancer (clinicaltrials.gov) -  Aug 9, 2022   
    P1b/2,  N=95, Active, not recruiting, 
    Recruiting --> Active, not recruiting | N=254 --> 47 Recruiting --> Active, not recruiting | N=272 --> 95
  • ||||||||||  derazantinib (ARQ 087) / Basilea
    Journal:  Derazantinib: an investigational drug for the treatment of cholangiocarcinoma. (Pubmed Central) -  Jan 11, 2022   
    The clinical safety profile of derazantinib was well manageable and compared favorably to the FGFR inhibitor class, particularly with a low incidence of drug-related hand-foot syndrome, stomatitis, retinal and nail toxicity. These findings support the need for increased molecular profiling of cholangiocarcinoma patients.
  • ||||||||||  derazantinib (ARQ 087) / Merck (MSD), Tecentriq (atezolizumab) / Roche
    Trial completion date, Trial primary completion date:  FIDES-02: Derazantinib and Atezolizumab in Patients With Urothelial Cancer (clinicaltrials.gov) -  Jul 21, 2021   
    P1b/2,  N=272, Recruiting, 
    Derazantinib showed clinically meaningful efficacy with durable objective responses, and a manageable safety profile with a particularly low incidence of drug-related hand-foot syndrome, stomatitis, retinal or nail toxicity in pts with iCCA harboring FGFR2fus. Trial completion date: May 2022 --> Oct 2023 | Trial primary completion date: Apr 2022 --> Jul 2023
  • ||||||||||  Clinical, Review, Journal:  FGFR Inhibitors in Oncology: Insight on the Management of Toxicities in Clinical Practice. (Pubmed Central) -  Jul 4, 2021   
    Along with these agents, many phase II/III clinical trials are currently evaluating the use of derazantinib, infigratinib, and futibatinib either alone or in combination with immunotherapy...In addition, we proposed treatment guidelines for the management of FGFR-inhibitor-associated toxicities. This work would invariably help practicing oncologists to effectively manage the unique toxicities of FGFR inhibitors.
  • ||||||||||  derazantinib (ARQ 087) / Basilea
    Journal:  Probing the Effects of the FGFR-Inhibitor Derazantinib on Vascular Development in Zebrafish Embryos. (Pubmed Central) -  Jan 6, 2021   
    For this purpose, we used the developing vasculature in the zebrafish embryo as a model system for angiogenesis in vivo. We show that DZB interferes with multiple angiogenic processes that are linked to FGF and VEGF signalling, revealing a potential dual role for DZB as a potent anti-angiogenic treatment.