Trestolone

[2][3] It has been under development for potential use as a male hormonal contraceptive and in androgen replacement therapy for low testosterone levels.[4][3] Trestolone is not a substrate for 5α-reductase and hence is not potentiated or inactivated in so-called "androgenic" tissues like the skin, hair follicles, and prostate gland.[6][13] However, trestolone has only weak estrogenic activity and an amount that would appear to be insufficient for replacement purposes, as evidenced by decreased bone mineral density in men treated with it for hypogonadism.In order to render a man infertile, a hormone-based male contraceptive method must stop spermatogenesis by interrupting the release of gonadotropins from the pituitary gland.[4][3] As a result of trestolone's gonadotropin-suppressing qualities, levels of serum testosterone fall sharply in men treated with sufficient amounts of the medication.Normally, an inadequate testosterone level causes undesirable effects such as fatigue, loss of skeletal muscle mass, reduced libido, and weight gain.[8][21] Development of trestolone for potential use in male hormonal contraception and androgen replacement therapy was started by 1993, and continued thereafter.
TestoloneTrenboloneRoutes ofadministrationSubcutaneous implantintramuscular injectiontrestolone acetateDrug classAndrogenAnabolic steroidProgestogenAntigonadotropinATC codeIUPAC nameCAS NumberDrugBankChemSpiderCompTox DashboardECHA InfoCardFormulaMolar massSMILESexperimentalhormonal birth control for menandrogen replacement therapylow testosterone levelsimplant that is placed into fatandrogen esterprodruginjection into muscleSide effectsagonistandrogen receptorbiological targettestosteroneprogestinsyntheticprogesterone receptorprogesteroneantigonadotropicsperm productioncontraceptivePopulation Councilnon-profitnon-governmental organizationreproductive healthmale hormonal contraceptivesexual dysfunctiondecreased sex drivereduced erectile functionbone mineral densityestrogen deficiencyandrogensdihydrotestosteronesubstrate5α-reductasetissueshair folliclesprostate glandanabolicandrogenicaromataseestrogen7α-methylestradiolmetaboliteestrogenicpotentprogestogenicNandroloneligandsaldosteronecortisolSpermatozoatestesspermatogenesisgonadotropinspituitary glandluteinizing hormonefollicle stimulating hormoneoligozoospermiaazoospermiasecondary sex characteristicsfatigueskeletal musclelibidopharmacokineticbioavailabilityelimination half-lifeoral administrationparenterallytransdermal patchtopical gelList of androgens/anabolic steroidsestranesteroidderivativemethyl group7α-methyl-19-norandrostenedioneandrogen prohormonedimethandrolonemiboleronedimethyltrienolonetibolonemale hormonal contraceptiongeneric namemodulators4-Androstenediol4-Dehydroepiandrosterone (4-DHEA)4-Hydroxytestosterone5-Androstenedione11-Ketotestosterone11β-HydroxyandrostenedioneAdrenosterone (11-ketoandrostenedione, 11-oxoandrostenedione)Androstenediol (5-androstenediol)Androstenediol 3β-acetateAndrostenediol 17β-acetateAndrostenediol diacetateAndrostenediol dipropionateAndrostenedione (4-androstenedione)AtamestaneBoldenoneBoldenone undecylenateBoldione (1,4-androstadienedione)ClostebolClostebol acetateClostebol caproateClostebol propionateCloxotestosteroneCloxotestosterone acetateDehydroandrosteroneDHEA (androstenolone, prasterone; 5-DHEA)DHEA enanthate (prasterone enanthate)DHEA sulfateExemestaneFormestanePlomestaneQuinboloneSilandrone+dutasteridePolytestosterone phloretin phosphate1-Androstenediol1-Androstenedione1-Androsterone (1-andro, 1-DHEA)1-Testosterone3α-Androstanediol5α-Androst-2-en-17-one7β-Hydroxyepiandrosterone11-KetodihydrotestosteroneAndrosteroneBolazineBolazine capronateDihydrofluoxymesteroneDihydrotestosterone (DHT)androstanolone, stanoloneDrostanoloneDrostanolone propionateEpiandrosteroneEpitiostanolMepitiostaneMesaboloneMesteroloneMesterolone cipionateMethyldiazinolNisterimeNisterime acetateProstanozolStenboloneStenbolone acetateTestifenon (testiphenon, testiphenone)7α-Methyl-19-norandrostenedione (MENT dione, trestione)11β-Methyl-19-nortestosterone11β-Methyl-19-nortestosterone dodecylcarbonate19-Nor-5-androstenediol19-Nor-5-androstenedione19-NordehydroepiandrosteroneBolandiolBolandiol dipropionateBolandione (19-nor-4-androstenedione)Bolmantalate (nandrolone adamantoate)DienedioneDienoloneDimethandrolone buciclateDimethandrolone dodecylcarbonateDimethandrolone undecanoateLS-1727 (nandrolone 17β-N-(2-chloroethyl)-N-nitrosocarbamate)Methoxydienone (methoxygonadiene)NorclostebolNorclostebol acetateNormethandrone (methylestrenolone, normethisterone)OxaboloneOxabolone cipionate (oxabolone cypionate)Trenbolone acetateTrenbolone enanthateTrenbolone hexahydrobenzylcarbonateTrenbolone undecanoateTrendioneTrestolone enanthate5α-Dihydronandrolone19-NorandrosteroneBolasteroneCalusteroneChlorodehydromethylandrostenediol (CDMA)Chlorodehydromethyltestosterone (CDMT)Chloromethylandrostenediol (CMA)EnestebolEthyltestosteroneFluoxymesteroneFormeboloneHydroxystenozoleMetandienone (methandrostenolone)Methandriol (methylandrostenediol)Methandriol bisenanthoyl acetateMethandriol diacetateMethandriol dipropionateMethandriol propionateMethylclostebol (chloromethyltestosterone)Methyltestosterone+esterified estrogensMethyltestosterone 3-hexyl etherOxymesteronePenmesterolTiomesteroneAndroisoxazoleDesoxymethyltestosteroneFurazabolMebolazine (dimethazine)MestanoloneMetenoloneMetenolone acetateMetenolone enanthateMethasteroneMethyl-1-testosteroneMethylepitiostanolMethylstenboloneOxandroloneOxymetholoneStanozololBolenolDimethyldienoloneEthyldienoloneEthylestrenolMethyldienoloneMethylhydroxynandrolone (MOHN, MHN)MetriboloneNorboletoneNorethandrolonePropetandrolRU-2309Tetrahydrogestrinone5α-Dihydronorethandrolone5α-DihydronormethandroneNorvinisterone (vinylnortestosterone)VinyltestosteroneDanazolEthinylandrostenediolEthandrostateEthisterone (ethynyltestosterone)17α-Ethynyl-3α-androstanediol17α-Ethynyl-3β-androstanediolDihydroethisteroneΔ4-TiboloneDesogestrelEtonogestrelEtynodiolEtynodiol diacetateGestodeneGestrinoneLevonorgestrelLevonorgestrel esterslevonorgestrel butanoateLynestrenolLynestrenol phenylpropionateNorethisteroneNorethisterone estersnorethisterone acetatenorethisterone enanthateNorgestrelNorgestrienoneQuingestanolQuingestanol acetate5α-Dihydrolevonorgestrel5α-Dihydronorethisterone6α-MethylprogesteroneMedroxyprogesterone acetateMegestrol acetate3-Keto-5α-abiraterone5α-AndrostaneAlternariolCl-4AS-1DrupanolTrilostaneZM-182345ACP-105AC-262,536AcetothiolutamideAcetoxolutamideAndarine (acetamidoxolutamide, androxolutamide, GTx-007, S-4)BMS-564,929Enobosarm (ostarine, MK-2866, GTx-024, S-22)GLPG-0492GSK2881078GSK-4336ALG121071 (LGD-121071)LGD-2226LGD-2941 (LGD-122941)LGD-3303LGD-4033JNJ-26146900JNJ-28330835JNJ-37654032OPK-88004 (LY-2452473, TT-701)PF-06260414RU-59063S-40503VosilasarmMK-0773TFM-4AS-17α-Thioprogesterone7α-Thiospironolactone7α-Thiomethylspironolactone11α-Hydroxyprogesterone15β-Hydroxycyproterone acetateAbirateroneAbiraterone acetateAllyltestosteroneBenorteroneCanrenoic acidCanrenoneChlormadinone acetateClascoteroneClometeroneCyproheptadineCyproteroneCyproterone acetateDelanteroneDelmadinone acetateDicirenoneDienogestDrospirenoneDU-41165EdogestroneEM-5854EpitestosteroneGaleteroneGuggulsteroneMedrogestoneMespirenoneMetogestMexrenoneMifepristoneNomegestrol acetateNordinoneOsateroneOsaterone acetateOxendolonePotassium canrenoatePromegestoneProrenoneRosteroloneSC-5233 (spirolactone)SpironolactoneSpirorenoneSpiroxasoneTopteroneTrimegestoneTrimethyltrienolone (R-2956)Zanoterone5N-BicalutamideApalutamideAtraric acidBakuchiolBavdegalutamideBicalutamideBisphenolsbisphenol Abisphenol Fbisphenol SBMS-641988CimetidineCioteronelCyanonilutamideDarolutamidep,p’-DDEDieldrinEndosulfanEnzalutamideEPI-001FenarimolFlutamideHydroxyflutamideInocoteroneInocoterone acetateKetoconazoleKetodarolutamideLavender oilLG-120907LinuronMasofanitenMethiocarbN-DesmethylapalutamideN-DesmethylenzalutamideNilutamidePentomonePhenothrinProchlorazProcymidoneProxalutamidePyrilutamideRalaniten (EPI-002)Ralaniten acetate (EPI-506)RD-162RezvilutamideRU-22930RU-56187RU-57073RU-58642RU-58841SeviteronelThalidomideTopilutamide (fluridil)Valproic acidVinclozolinGPRC6ACationsaluminiumcalciumgadoliniummagnesiumstrontiumEstradiolL-α-Amino acidsL-arginineL-lysineL-ornithineOsteocalcinList of androgens and anabolic steroidsEstrogen receptor2-Hydroxyestradiol2-Hydroxyestrone3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol3α-Hydroxytibolone3β-Hydroxytibolone3β-Androstanediol4-Androstenedione4-Fluoroestradiol4-Hydroxyestradiol4-Hydroxyestrone4-Methoxyestradiol4-Methoxyestrone5-Androstenediol7-Oxo-DHEA7α-Hydroxy-DHEA8,9-Dehydroestradiol8,9-Dehydroestrone8β-VE210β,17β-Dihydroxyestra-1,4-dien-3-one (DHED)11β-Chloromethylestradiol11β-Methoxyestradiol15α-Hydroxyestradiol16-Ketoestradiol16-Ketoestrone16α-Fluoroestradiol16α-Hydroxy-DHEA16α-Hydroxyestrone16α-Iodoestradiol16α-LE216β-Hydroxyestrone16β,17α-Epiestriol (16β-hydroxy-17α-estradiol)17α-Estradiolalfatradiol17α-Dihydroequilenin17α-Dihydroequilin17α-Epiestriol (16α-hydroxy-17α-estradiol)17β-Dihydroequilenin17β-Dihydroequilin17β-Methyl-17α-dihydroequileninAlestramustineAlmestroneAnabolic steroidsAtrimustineButolameClomestroneCloxestradiolCloxestradiol acetateConjugated estriolConjugated estrogensCyclodiolCyclotriolDHEA-Sent-EstradiolEpiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol)EpimestrolEquileninEquilinERA-63 (ORG-37663)Esterified estrogensEstetrolLipoidal estradiolPolyestradiol phosphateEstramustineEstramustine phosphateEstrapronicateEstrazinolEstriolPolyestriol phosphateEstrofurateEstrogenic substancesEstromustineEstroneEstrone methyl etherEstropipateEtamestrol (eptamestrol)EthinylestradiolEthinylestradiol 3-benzoateEthinylestradiol sulfonateEthinylestriolEthylestradiolHexolameHippulinHydroxyestrone diacetateMestranolMethylestradiolMoxestrolMytatrienediolNilestriolNoretynodrelOrestratePentolameProdiameProlamePromestrieneRU-16117QuinestradolQuinestrol(R,R)-THC(S,S)-THC2,8-DHHHCβ-LGND2 (GTx-878)AllenestrolAllenolic acidBenzestrolBifluranolBisdehydrodoisynolic acidButestrolCarbestrolD-15414DCW234DiarylpropionitrileDienestrolDienestrol diacetateDiethylstilbestrolDimestrol (dianisylhexene)DimethylstilbestrolDoisynoestrol (fenocycline)Doisynolic acidEfavirenzElacestrantERB-196 (WAY-202196)Erteberel (SERBA-1, LY-500307)Estrobin (DBE)FenestrelFERb 033Fosfestrol (diethylstilbestrol diphosphate)Furostilbestrol (diethylstilbestrol difuroate)GTx-758HexestrolICI-85966 (Stilbostat)meso-Butestrolmeso-HexestrolMestilbolMethallenestrilMethestrolMethestrol dipropionateParoxypropionePentafluranolPhenestrolPrinaberel (ERB-041, WAY-202041)PropylpyrazoletriolQuadrosilanSC-4289SERBA-2SKF-82,958TerfluranolTriphenylbromoethyleneTriphenylchloroethyleneTriphenyliodoethyleneTriphenylmethylethylene (triphenylpropene)WAY-166818WAY-200070WAY-204688 (SIM-688)WAY-214156ERB-26ERA-45ERB-79ZK-283197anetholedianetholedianolphotoanetholeChalconoidsisoliquiritigeninphloretinphlorizin (phloridzin)wedelolactoneCoumestanscoumestrolpsoralidinFlavonoids7,8-DHF8-prenylnaringeninapigeninbaicaleinbaicalinbiochanin AcalycosincatechindaidzeindaidzinepicatechinformononetinglabreneglabridingenisteingenistinglyciteinkaempferolliquiritigeninmirificinmyricetinnaringeninpinocembrinprunetinpuerarinquercetintectoridintectorigeninLignansenterodiolenterolactonenyasol (cis-hinokiresinol)MetalloestrogenscadmiumPesticidesmethoxychlortriclocarbantriclosanPhytosteroidsdigitoxindigitalisdiosgeninPhytosterolsβ-sitosterolcampesterolstigmasterolResorcylic acid lactoneszearalanoneα-zearalenolβ-zearalenolzearalenonezeranol (α-zearalanol)taleranol (teranol, β-zearalanol)deoxymiroestrolmiroestrolStilbenoidsresveratrolrhaponticinSynthetic xenoestrogensalkylphenolsparabensphthalatesagnuside2-Phenylbenzofuran4'-Hydroxynorendoxifen27-HydroxycholesterolAcefluranolAcolbifeneAfimoxifeneAnordiolAnordrinArzoxifeneBazedoxifeneBrilanestrantBroparestrolCamizestrantChlorotrianiseneClomifeneClomifenoxideCyclofenilDesmethylchlorotrianiseneDroloxifeneEnclomifeneEndoxifenEtacstil (GW-5638, DPC-974)Ethamoxytriphetol (MER-25)FemarelleFispemifeneICI-55548IdoxifeneLasofoxifeneLevormeloxifeneLN-1643LN-2299MenerbaMiproxifeneMiproxifene phosphateNafoxidineNitromifeneNNC 45-0095OrmeloxifeneOspemifenePanomifenePipendoxifeneRaloxifeneRimostil (P-081)TamoxifenTAS-108 (SR-16234)ToremifeneTrioxifeneZindoxifeneZuclomifene7β-Hydroxy-DHEACytestrol acetateFulvestrant (ICI-182780)GlyceollinsICI-164384MethylpiperidinopyrazolePhenytoinERX-112-MethoxyestradiolAfimoxifene (4-hydroxytamoxifen)Atrazinep,p'-DDTHydroxytyrosolKeponeNicotinic acidNicotinamideNonylphenolOleuropeinList of estrogens3β-Dihydroprogesterone5α-Dihydroprogesterone9α-Bromo-11-ketoprogesterone11-Dehydroprogesterone11-Deoxycorticosterone16α-Hydroxyprogesterone20α-Dihydroprogesterone20β-DihydroprogesteroneDimepregnenP1-185Progesterone 3-acetyl enol etherQuingestrone20α-Dihydrodydrogesterone20α-DihydrotrengestoneDU-41164DydrogesteroneRetroprogesteroneRo 6-3129Trengestone6α-Methyl-17α-bromoprogesterone16-Methylene-17α-hydroxyprogesterone acetate17α-Bromoprogesterone17α-Hydroxyprogesterone (hydroxyprogesterone)17α-MethylprogesteroneAcetomepregenol (mepregenol diacetate)AlgestoneAlgestone acetonideAlgestone acetophenideAnagestoneAnagestone acetateBromethenmadinone acetateButagest (buterol)ChlormadinoneChlormadinone caproateChlormethenmadinone acetateCismadinoneCismadinone acetateClogestoneClogestone acetateClomegestoneClomegestone acetateCymegesolateDelmadinoneFlugestoneFlugestone acetateFluorometholoneFluorometholone acetateFlumedroxoneFlumedroxone acetateFluoromedroxyprogesterone acetateGestacloneHaloprogesteroneHydromadinoneHydromadinone acetateHydroxyprogesterone acetateHydroxyprogesterone caproate (hydroxyprogesterone hexanoate)Hydroxyprogesterone heptanoate (hydroxyprogesterone enanthate)Hydroxyprogesterone heptanoate benzilic acid hydrazoneMecigestone (pentarane B)MedroxyprogesteroneMedroxyprogesterone caproateMegestrolMegestrol caproateMelengestrolMelengestrol acetateMethenmadinoneMethenmadinone acetateMethenmadinone caproateMometasoneMometasone furoatePentagestronePentagestrone acetatePentarane AProligestoneTriamcinolone acetonide17α-Methyl-19-norprogesterone18-Methylsegesterone acetate19-NorprogesteroneAmadinoneAmadinone acetateDemegestoneGestadienolGestadienol acetateGestonorone acetate (gestronol acetate)Gestonorone caproate (gestronol hexanoate)Gestronol (gestonorone)NomegestrolNorgestometORG-2058OxogestoneOxogestone phenpropionate (xinogestone)SegesteroneSegesterone acetate (nestorone)6,6-Difluoronorethisterone6,6-Difluoronorethisterone acetate17α-Allyl-19-nortestosteroneAllylestrenolAltrenogestChloroethynylnorgestrelCingestolEthisteroneEthyneroneMetynodiolMetynodiol diacetateNorelgestrominNorethisterone (norethindrone)NorgesteroneNorgestimateNorvinisteroneTigestolTosagestinBolandioneDimethisteroneEthylestrenol (ethylnandrol)Metribolone (R-1881)Nandrolone estersnandrolone decanoatenandrolone phenylpropionateNormethandrone (methylestrenolone, normethandrolone, normethisterone)Trenbolone (trienolone)Trenbolone estersSC-81093,8-DihydrodiligustilideLG-2527RiligustilideTanaprogetORG-47241ORG-201745AsoprisnilAsoprisnil ecamateMetapristone (RU-42633)Mifepristone (RU-486)ORF-9326TelapristoneUlipristal acetateVilaprisanSyringic acidAglepristoneLilopristoneLonaprisanOnapristoneToripristone5β-Dihydroprogesterone11-Deoxycortisone (21-hydroxyprogesterone)11-Deoxycortisol (17α,21-dihydroxyprogesterone)17α-HydroxyprogesteroneAllopregnanolonePregnenoloneList of progestogens