ArticleMolecules (Basel, Switzerland)2022
Metabolite Identification of a Novel Anti-Leishmanial Agent OJT007 in Rat Liver Microsomes Using LC-MS/MS.
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 8 citations in OpenAlex.
- The effect of pH stability and aqueous solubility on the oral bioavailability of a novel antileishmanial agent.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2026Article
- Drug Metabolism and Pharmacokinetic Evaluation of a Novel RNase H2 Inhibitor for the Treatment of Triple-Negative Breast Cancer.Pharmaceutics · 2025Article
- Metabolite Identification of Isopropoxy Benzene Guanidine in Rat Liver Microsomes by Using UHPLC-Q-TOF-MS/MS.International journal of molecular sciences · 2023Article
- Structural Investigation of Betulinic Acid Plasma Metabolites by Tandem Mass Spectrometry.Molecules (Basel, Switzerland) · 2022Article
- PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education.Pharmacology research & perspectives · 2022Article
- A Comprehensive Study to Identify Major Metabolites of an Amoxicillin-Sulbactam Hybrid Molecule in Rats and Its Metabolic Pathway Using UPLC-Q-TOF-MS/MS.Metabolites · 2022Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The purpose of this study was to identify potential metabolic pathways and metabolites of OJT007, a methionine aminopeptidase 1 (MetAP1) inhibitor. OJT007 is a novel drug with potent antiproliferative effects against Leishmania Major. We conducted in vitro Phase I oxidation and Phase II glucuronidation assays on OJT007 using rat liver microsomes. Four unknown metabolites were initially identified using a UPLC-UV system from microsomal incubated samples. LC-MS/MS analysis was then used to identify the structural characteristics of these metabolites via precursor ion scan, neutral loss scan, and product ion scan. A glucuronide metabolite was further confirmed by β-glucuronidase hydrolysis. The kinetic parameters of OJT007 glucuronidation demonstrated that OJT007 undergoes rapid metabolism. These results demonstrate the liver's microsomal ability to mediate three mono-oxidated metabolites and one mono-glucuronide metabolite. This suggests hepatic glucuronidation metabolism of OJT007 may be the cause of its poor oral bioavailability.
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Registered trials
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