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DRUG:

Qapzola (apaziquone)

i
Other names: EO9, NOR 701, NSC 382459
Associations
Trials
Company:
Assertio
Drug class:
DNA cross linking agent
Associations
Trials
2d
Molecular understanding for therapeutic targeting of hypoxia in breast cancer. (PubMed, Expert Opin Ther Targets)
Apart HIF itself, other potential molecular targets such as prolyl-hydroxylases (PHD), von Hippel-Lindau protein (VHL), monocarboxylate transporters (MCTs), Na+ /H+ exchangers (NHEs), vacuolar ATPases (V-ATPase), anion exchangers (AEs), Na+ /HCO₃- co-transporters (NBCs), vascular endothelial growth factor (VEGF) and carbonic anhydrases were identified as being involved in tumorigenesis. HIF-1α inhibitors (topotecan, digoxin, PX-478), hypoxia-activated prodrugs (evofosfamide, apaziquone, porfiromycin, tirapazamine, banoxantrone) and carbonic anhydrase IX/XII inhibitors (SLC-0111) are either used clinically or in clinical development for the management of hypoxic breast cancers.
Review • Journal
|
HIF1A (Hypoxia inducible factor 1, alpha subunit) • CA9 (Carbonic anhydrase 9)
|
topotecan • evofosfamide (IMGS-101) • PX-478 • Qapzola (apaziquone) • SLC-0111 • Tirazone (tirapazamine)
4years
Development of Hif1a Pharmacogenomic Mutation Models to Study Individual Variations in Drug Action for Tumor Hypoxia: An in Silico Approach. (PubMed, J Pharm Bioallied Sci)
Potential models were used for interaction studies with hypoxia-specific molecules (tirapazamine, apaziquone, and ENMD) using docking analysis. It also elucidates that the therapeutic effect is altered concerning population-dependent genetic changes in the individual. The study, therefore, asserts the need to set up a personalized drug design approach to enhance tumor hypoxia treatment efficacy.
Journal
|
HIF1A (Hypoxia inducible factor 1, alpha subunit)
|
Qapzola (apaziquone) • Tirazone (tirapazamine)