Myovant qhov ncauj GnRH receptor antagonist relugolix nkag mus rau kev kuaj xyuas qhov muaj feem thib hauv Asmeskas: kev tshem tawm tus nqi siab txog 96.7%

Myovant Sciences yog lub tuam txhab kho mob tsom rau kev tsim kho tshiab rau cov poj niam' s kev noj qab haus huv thiab mob prostate. Tsis ntev los no, lub tuam txhab tshaj tawm tias US Food and Drug Administration (FDA) tau lees txais cov ntawv thov tshuaj tshiab niaj hnub (NDA) rau tshuaj tiv thaiv kab mob hauv lub qhov ncauj (120mg) rau kev kho mob ntawm kev mob qog nqaij hlav prostate thiab tau txais kev tshuaj xyuas ua ntej. Tus nqi siv tshuaj rau cov neeg siv tshuaj (PDUFA) lub hom phiaj Hnub Nws' s Lub Kaum Ob Hlis 20, 2020. Hauv qhov kev tshawb pom theem III HERO, tus nqi kho dua ntawm relugolix tau txog 96.7%, uas zoo tshaj li leuprolide acetate, thiab cov txoj kev pheej hmoo ntawm cov kab mob plawv loj tau raug txo los ntawm 54%.

Hauv tsab ntawv lees txais, FDA tau hais tias tam sim no nws tsis xav nrhiav tus neeg pab tswv yim lub rooj sib tham ntawm NDA. Yog tias tau txais kev pom zoo, relugolix yuav yog thawj zaug thiab tsuas yog qhov ncauj gonadotropin-tso cov tshuaj hormones (GnRH) receptor antagonist rau kev kho tus mob qog nqaij hlav hauv prostate.

Relugolix yog ib zaug ib hnub, qhov ncauj GnRH receptor antagonist uas inhibits testosterone ntau lawm, yam tshuaj uas tuaj yeem txhawb kev loj hlob ntawm kev mob qog nqaij hlav prostate. Ntxiv rau, relugolix kuj tseem tuaj yeem txo qis ntawm zes qe menyuam estradiol los ntawm kev thaiv GnRH receptor nyob rau hauv lub caj pas pituitary, cov tshuaj hormone paub los txhawb kev loj hlob ntawm uterine fibroids thiab endometriosis.

Tam sim no, Myovant Sciences tab tom tab tom txhim kho qhov ncauj relugolix ntsiav tshuaj (120mg) ib hnub ib zaug rau kev kho mob cancer prostate siab heev. Tsis tas li ntawd, lub tuam txhab tseem tab tom tsim kho ib zaug txhua hnub qhov ncauj relugolix compound ntsiav tshuaj (relugolix 40mg, estradiol 1.0mg, norethisterone acetate 0.5mg) los kho tus poj niam uterine fibroids thiab endometriosis. Nyob rau lub Peb Hlis thiab Lub Rau Hli ntawm lub xyoo no, Myovant Sciences tau xa daim ntawv thov kev lag luam ntawm relugolix compound ntsiav tshuaj mus rau European Chaw Tshuaj Tshuaj (EMA) thiab FDA, feem, rau kev kho mob me ntsis mus rau cov tsos mob hnyav ntawm cov poj niam nrog uterine fibroids. Ob qhov tsos mob tshwm sim ntawm uterine fibroids yog cov ntshav tawm los hnyav (HMB) thiab mob. Yog tias tau txais kev pom zoo, relugolix compound ntsiav tshuaj yuav muab kev kho mob ib hnub rau cov neeg mob poj niam uas muaj uterine fibroids.

NDA ntawm relugolix nyob rau hauv kev kho mob ntawm kev mob qog nqaij hlav prostate siab tshaj yog ua raws li cov txiaj ntsig tau zoo ntawm Kev Tshawb Fawb III HERO. Qhov no yog randomized, qhib-daim ntawv lo, cov pab pawg sib law liag, ntau lub teb chaws chaw tshawb fawb sib piv sib piv relugolix thiab leuprolide acetate ntau dua li 900 tus neeg mob androgen rhiab uas yuav tsum tau tsawg kawg ib xyoos ntawm kev kho mob androgen deprivation txuas ntxiv (ADT) Tau tsim tawm hauv cov neeg mob uas muaj prostate siab heev. mob cancer. Hauv txoj kev tshawb nrhiav, cov neeg mob tau muab faib rau hauv 2: 1 piv thiab tau txais relugolix (ib koob ntawm 360 mg loading, tom qab 120 mg ib zaug ib hnub) lossis leuprolide acetate pas dej tso tawm (ib zaug hauv lub Peb Hlis).

Cov txiaj ntsig tau pom tias relugolix tau mus txog qhov pib kev ua tau zoo: thaum 48 lub lim tiam ntawm kev kho mob, 96.7% ntawm cov txiv neej hauv pawg relugolix tau ua tiav cov tshuaj loog testosterone nyob rau qib castration (GG lt; 50ng / dL), piv nrog 88.8% hauv leuprolide acetate kev kho mob pab pawg.

Ntxiv rau, relugolix kuj tau mus txog rau 6 qhov tseem ceeb tshaj plaws theem kawg (p qhov tseem ceeb< 0.0001),="" qhia="" tau="" tias="" nws="" zoo="" dua="" rau="" leuprolide="" acetate="" nyob="" rau="" hauv="" cov="" nqe="" lus="" ntawm="" kev="" thim="" sai="" thiab="" sib="" sib="" zog="" nqus="" tshuaj="" testosterone,="" psa="" teb,="" thiab="" testosterone="" rov="" qab="" tom="" qab="" kev="" kho="" mob.="" tag="" nrho="" qhov="" tshwm="" sim="" ntawm="" qhov="" tsis="" zoo="" hauv="" pawg="" relugolix="" thiab="" pawg="" leuprolide="" acetate="" pawg="" tau="" sib="" piv="" (92.9%="" vs="" 93.5%).="" hais="" txog="" cov="" teeb="" meem="" loj="" ntawm="" cov="" hlab="" plawv="" (mace),="" cov="" thim="" rov="" qab="" pab="" pawg="" muaj="" qhov="" pheej="" hmoo="" tsawg="" dua="" 54%="" piv="" rau="" cov="" pab="" pawg="" leuprolide="" acetate="" (qhov="" tshwm="" sim:="" 2.9%="" vs="" 6.2%).="" cov="" xwm="" txheej="" no="" suav="" nrog="" kev="" tsis="" ua="" kom="" tsis="" mob="" ntshav="" qab="" zib,="" tsis="" mob="" ntshav="" siab="" thiab="" tuag="" tsis="" taus="" thiab="" txhua="" yam="" vim="" muaj="" kev="" tuag.="" ntawm="" cov="" txiv="" neej="" muaj="" keeb="" kwm="" ntawm="" mace,="" relugolix="" pawg="" muaj="" 80%="" kev="" txo="" qis="" hauv="" mace="" cov="" xwm="" txheej="" piv="" nrog="" leuprolide="" acetate="" pawg="" (3.6%="" vs="" 17.8%).="" lwm="" lub="" ntsiab="" lus="" kawg="" txuas="" ntxiv="" rau="" txoj="" kev="" tshawb="" no,="" lub="" sijhawm="" ua="" si-lub="" sijhawm="" tiv="" thaiv="" kev="" mob,="" yuav="" tsum="" tau="" txais="" nyob="" rau="" peb="" lub="" hlis="" thib="" peb="" ntawm="">

Relugolix cov qauv tshuaj lom neeg thiab cov txheej txheem ntawm kev ua (Tau qhov tseeb ntawm cov qauv txheej txheem: medchemexpress.com)

Relugolix tau tsim los ntawm Takeda, thiab Myovant Sciences (ib lub tuam txhab tsim los ntawm Roivant thiab Takeda) tau txais daim ntawv tso cai thoob ntiaj teb nyob rau lub Rau Hli 2016 tsuas yog Nyij Pooj thiab lwm lub teb chaws Asia. Hauv Nyij Pooj, relugolix tau txais kev pom zoo thaum Lub Ib Hlis 2019 thiab tau ua lag luam nyob hauv cov lag luam muaj npe hu ua Relumina txhawm rau txhim kho cov tsos mob hauv qab no tshwm sim los ntawm uterine fibroids: menorrhagia, mob plab qis, mob nraub qaum, thiab mob ntshav tsis txaus.

Hauv tebchaws Asmeskas, kab mob prostate yog qhov mob cancer thib ob hauv cov txiv neej thiab yog qhov thib ob ua rau ploj tuag rau txiv neej. Kev mob plawv yog qhov uas ua rau muaj kev tuag rau cov txiv neej mob qog nqaij hlav cancer, uas yog li 34% ntawm cov txiv neej mob qog nqaij hlav cancer. Advanced prostate cancer yog hais txog tus mob prostate uas tau kis lossis rov huam mob tom qab kho tas. Nws yuav suav nrog cov txiv neej muaj biochemical kev mob rov qab (PSA ntau ntxiv thaum tsis muaj metastatic kab mob los ntawm kev ntsuas duab), kab mob hauv zos siab, lossis kab mob metastatic. Kev kho mob ntawm kev kho mob qog nqaij hlav prostate feem ntau suav nrog androgen kev tiv thaiv kab mob (ADT), uas txo cov testosterone kom tsawg heev, feem ntau hu ua qib castration. Gonadotropin-tso cov tshuaj hormones (GnRH) receptor agonists, xws li leuprolide acetate lossis txhawb kev txhaj tshuaj, yog tam sim no tus qauv kev saib xyuas rau androgen deprivation txoj kev kho (ADT). Txawm li cas los xij, GnRH receptor agonists tuaj yeem cuam tshuam nrog kev txiav txim siab txog mechanism, suav nrog qhov pib muaj kev phom sij hauv qib testosterone, uas yuav ua rau muaj kev puas siab hauv cov chaw kuaj mob ntau (piv txwv li, kev kho mob lossis tshuaj tua ntshav hormonal), thiab ncua testosterone rov qab los tom qab tshem tawm yeeb tshuaj.