DSP-1053 / Sumitomo Pharma - LARVOL DELTA

Application of CYP1A2-Template System to Understand Metabolic Processes in the Safety Assessment. (PubMed, Food Saf (Tokyo)) - "Simulation experiments of a topoisomerase-targeting agent, amonafide, offered a possible new inhibitory-mechanism as Trigger-residue inactivation on human CYP1A2 Template...The mechanism was also supported on the inhibition/inactivation of two other drugs, DSP-1053 and binimetinib...These results suggest that CYP Template systems developed are effective tools to warn an appearance of unstable reactive intermediates. Our CYP-Template systems would support confident judgements in safety assessments through offering the mechanistic understandings of the metabolism."

Journal • CYP1A2

A Multiple Ascending Oral Dose Evaluation of the Safety, Tolerability, and Pharmacokinetics of DSP-1053 and Its Metabolites in Healthy Subjects and in Subjects With Major Depressive Disorder (clinicaltrials.gov) - P1; N=64; Active, not recruiting; Sponsor: Sunovion; Recruiting -> Active, not recruiting

Enrollment closed • Acute Coronary Syndrome • Biosimilar • Chronic Kidney Disease • Heart Failure • Hepatitis C Virus • Immunology • Myositis • Pain

Time-dependent inhibition (TDI) of CYP1A2 by a CYP3A4-mediated reactive metabolite: Proposal for a Novel mechanism of irreversible TDI by a non-suicide substrate. (PubMed, Xenobiotica) - "4. In conclusion, a possible mechanism for DSP-1053 TDI of CYP1A2 is that DSP-1053 iminium ion, which is generated by CYP3A4, departs from CYP3A4 without inhibiting it and covalently binds to CYP1A2."

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