Trilostane
[6][7][8][9][1] It was withdrawn for use in humans in the United States in the 1990s[10] but was subsequently approved for use in veterinary medicine in the 2000s to treat Cushing's syndrome in dogs.[1] Serious gastrointestinal side effects of trilostane alone or in combination with an NSAID like peptic ulcer, erosive gastritis, gastric perforation, hematemesis, and melena may occur in some individuals.[1] In addition to steroidogenesis inhibition, trilostane has been found to act as a noncompetitive antiestrogen, via direct and presumably allosteric interactions with the estrogen receptor.[10][24][25][26] Trilostane was approved in the United States in 2008 for the treatment of Cushing's disease (hyperadrenocorticism) in dogs under the brand name Vetoryl.[2] In March 2024, the CVMP adopted a positive opinion, recommending the granting of a marketing authorization for the veterinary medicinal product Trilorale, oral suspension for dogs.[6][7] Trilostane has been marketed under a number of brand names including Desopan, Modrastane, Modrenal, Trilox, Vetoryl, Oncovet TL and Winstan.[26][31] Success was measured by improvements in both blood test results and physical symptoms (normalized appetite and activity level, and decreased panting, thirst, and urination).
Routes ofadministrationBy mouthATC codeH02CA01QH02CA01Legal status ℞-only℞-onlyPharmacokineticMetabolismMetabolitesElimination half-lifeIUPAC nameCAS NumberIUPHAR/BPSDrugBankChemSpiderChEMBLCompTox DashboardECHA InfoCardFormulaMolar massSMILESCushing's syndromeConn's syndromepostmenopausalbreast cancerwithdrawnUnited Statesveterinary medicinecorticosteroidglucocorticoid deficiencypregnantkidneyliver diseasecardiovascular diseasenursingSide effectsgastrointestinalgastritisnauseavomitingdiarrheaNonsteroidal antiinflammatory drugspeptic ulcererosive gastritisgastric perforationhematemesismelenagranulocytopeniaparesthesiaSteroidogenesissteroidogenesis inhibitorinhibitor3β-hydroxysteroid dehydrogenasehydroxysteroidspregnenolone17α-hydroxypregnenolonedehydroepiandrosteroneandrostenediolketosteroidsprogesterone17α-hydroxyprogesteroneandrostenedionetestosteroneproductionsteroid hormonesandrogensestrogensprogestogensglucocorticoidsmineralocorticoidsmechanism of actioncortisolaldosteroneadrenal glandsabortifacientaromatase inhibitorestroneestradiolnoncompetitiveantiestrogenallostericestrogen receptoragonistandrogen receptorprostate cancermetabolizedmetabolitereversibleelimination half-livesexcretedkidneyssyntheticandrostanesteroidderivative5α-reduced3α-androstanediol3β-androstanedioldihydrotestosteronesynthesisUnited KingdomCushing's diseaseAlopecia Xpituitaryadrenalselegilinemitotaneoff-labelcompounding pharmaciesgeneric namesafetyeffectivenessblood testappetitethirsturinationantiestrogensAlfatradiolanabolic steroidsmethyltestosteronemetandienoneprogestinsnorethisteronenoretynodrel