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Epacadostat (INCB024360) powder

mlingo:
5.00 kuchokera 5 kutengera 1 kasitomala mlingo
SKU: 1204669-58-8. Category:

AASraw ili ndi kaphatikizidwe ndi kapangidwe kameneka kuchokera ku gramu kupita ku kapangidwe ka Epacadostat (INCB024360) powder (1204669-58-8), pansi pa lamulo la CGMP ndi dongosolo loyendetsa khalidwe labwino.

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Video ya Epacadostat (INCB024360)


Epacadostat (INCB024360) Mafoda a mtundu

Name: Epacadostat (INCB024360) powder
CAS: 1204669-58-8
Makhalidwe a Maselo: C11H13BrFN7O4S
Kulemera kwa maselo: 438.23
Melt Point: 151-153 ° C
Kusungirako nyengo: -20 ° C Freezer
mtundu; Yoyera mpaka wofiira


Epacadostat (INCB024360) ufa mu ntchito

Mayina

Epacadostat ufa; IDO inhibitor 1; INCB 024360; 1204669-58-8; 1204669-37-3 INCB-024360

Ntchito yogwiritsa ntchito ufa wa Epacadostat

Epacadostat powder ndi mankhwala opezeka pamtundu wa hydroxyamidine ndi inhibitor ya indoleamine 2,3-dioxygenase (IDO1), yomwe imatha kugwira ntchito yoteteza thupi komanso kuteteza thupi. Zilonda zapacadostat ndipo zimamangiriza ku IDO1, nyamayi yomwe imayambitsa mchere wa tryptophan mu kynurenine. Mwa kuletsa IDO1 ndi kuchepa kwa kynurenine mu maselo otupa, INCB024360 ikuwonjezereka ndikubwezeretsa kuchulukitsa ndi kuyambitsa maselo osiyanasiyana a immune, kuphatikizapo maselo a dendritic (DCs), NK cells, ndi T-lymphocytes, komanso kuperewera kwa interferon (IFN), ndi kuchepetsa mu maselo otsogolera okhudza Tom (Tregs) ogwirizana ndi zotupa. Kugwiritsa ntchito chitetezo cha mthupi, chomwe chimadulidwa mu khansa zambiri, chingalepheretse kukula kwa IDO1-kutulutsa maselo otupa. IDO1 imadetsedwa kwambiri ndi mitundu yosiyanasiyana ya maselo otupa ndi DC.

Pulofini ya INCB024360 yayigwiritsidwa ntchito m'mayesero akuphunzira chithandizo cha HL, Melanoma, Glioblastoma, Mucosal Melanoma, ndi Ovarian Carcinoma, pakati pa ena.

Chenjezo pa INCB024360 ufa

Deta imabweretsa chikhulupiliro cha chikhulupiriro cha Incyte mu njira yogwiritsira ntchito Epacadostat powder. Mankhwalawa amatsitsa mavitamini a IDO1 kuti ateteze chitetezo cha mthupi. Nthenda ya epacadostat imachititsa kuti tizilombo toyambitsa matenda tizilumikizidwe, tipewe chitetezo cha mthupi kuti chigwire chotupacho ndi mphamvu yake yonse. Ngakhale kuti pali deta yambiri yofunikira kutsimikizira kuti chidziwitso, zomwe zikhoza kukhala ndi zovuta zokhudzana ndi msika wa immuno-oncology.

Deta ya Incyte imaphatikizapo bwino kuphatikizapo Bristol-Myers 'Opdivo ndi Yervoy, yomwe inagonjetsa FDA kuvomereza kumayambiriro kwa chaka chatha pothandizira mphamvu ya PFS ya miyezi 11.5 kwa odwala omwe ali ndi khansa yapamtunda.

Pali zifukwa zoganizira kusiyana pakati pa PFS ndi mayesero a zachipatala omwe potsirizira pake adzawamasulira m'mphepete mwa Incyte. Mlandu wa Bristol-Myers unalembetsa odwala omwe amachiritsidwa, pamene maphunziro ena a Incyte aperekedwa kale. Kuchuluka kwa mankhwala a Incyte ndikutenga mpata wofikira pakati pa PFS koma ndalama zomwe zapezeka pa miyezi isanu ndi umodzi, 12 ndi 18 zimati ndizopangitsa kuti opdivo-Yervoy izikhala bwino.

Incyte ikhoza kuwonetsanso kuti deta yosungira kuti muthe kutsutsana nayo ingakhale yabwino ya Bristol-Myers. Zotsatira zatsopano zomwe zidatchulidwa 17% za odwala zinachitikira katatu kapena zochitika zovuta zokhudzana ndi mankhwala. Izi zimagwirizanitsa ndi zotsatira zomwe zimaphatikizidwa ndi Bristol-Myers, omwe, polemba chaka chino, adalumikizidwa ku chiwerengero cha 58% cha zochitika zitatu kapena zinayi zosokoneza.

Maumboni ena

Epacadostat ufa ndi mankhwala a indoleamine 2,3-dioxygenase 1 (IDO1) okhala ndi IC50 mtengo wa 7.1 nM m'maselo a HeLa omwe amasonyeza ntchito pang'ono motsutsana ndi michere yokhudza IDO2 kapena tryptophan 2,3-dioxygenase (TDO) .1 Yasonyezedwa kuti ikulimbikitsa T ndi kupha maselo a chilengedwe, kuonjezera kupanga IFN-γ, ndi kuchepetsa kutembenuzika ku maselo ofanana a T (Treg) omwe ali m'chikhalidwe cha mtundu wa allogeneic lymphocytes omwe ali ndi maselo a dendritic kapena maselo a tumimba.XXMUMX Epacadostat ufa ikhozanso kuletsa chotupa kukula kwa mbewa zopweteka m'mimba mwa njira yodalirika.

Mlomo wamapezeka hydroxyamidine ndi inhibitor ya indoleamine 2,3-dioxygenase (IDO1), yomwe imatha kugwira ntchito yoteteza thupi komanso kuteteza thupi. Nkhumba za INCB024360 ndikumangiriza ku IDO1, enzyme yomwe imayambitsa mchere wa tryptophan mu kynurenine. Powononga IDO1 ndi kuchepa kwa kynurenine m'maselo otupa, kuwonjezeka kwa Epacadostat kukuwonjezereka ndi kubwezeretsa kuwonjezeka kwa maselo osiyanasiyana, kuphatikizapo maselo a dendritic (DCs), NK cells, ndi T-lymphocytes, komanso ma interferon (IFN). kuchepetsa maselo otsogolera a T ozungulira (Tregs) ogwirizana ndi zotupa. Kugwiritsa ntchito chitetezo cha mthupi, chomwe chimadulidwa mu khansa zambiri, chingalepheretse kukula kwa IDO1-kutulutsa maselo otupa. IDO1 imadetsedwa kwambiri ndi mitundu yosiyanasiyana ya maselo otupa ndi DC. Fufuzani mayesero okhudzana ndi ma ARV pogwiritsa ntchito wothandizira.

Indoleamine 2,3-dioxygenase 1 (IDO1) ndi chinsinsi chamadzimadzi omwe amachititsa kuti thupi lisamayambe kuteteza chitetezo cha m'thupi. Mafuta a epacadostat ndi kufufuzira, ndipamwamba kwambiri komanso yosankha mankhwala oletsa tizilombo toyambitsa matenda a IDO1 omwe amachititsa kuti tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda. Phunziro limodzi la manja, kuphatikiza kwa INCB024360 ufa ndi chitetezo cha mthupi chitetezo cha mthupi chawonetsetsa umboni wa odwala omwe ali ndi khansa yosakanirika kapena yamatenda. M'maphunzirowa, INCB024360 powder pamodzi ndi CTLA-4 inhibitor ipilimumab kapena PD-1 inhibitor KEYTRUDA mitengo yabwino yotsatila poyerekeza ndi kafukufuku wa chitetezo cha m'thupi chokha.

Kuphatikizira IDO inhibitor Epacadostat powder ndi nivolumab (Opdivo) inasonyeza zizindikiro zodalirika za ntchito kwa odwala squamous cell carcinoma a mutu ndi khosi (SCCHC) ndi omwe ali ndi khansa ya melanoma, malinga ndi zomwe apeza pa kafukufuku wa I / II ECHO-204 Msonkhano Wapachaka wa 2017 ASCO.

Kuphatikizidwa kunasonyeza kuti pangakhale mlingo woyenera (ORR) wa 63% ndi mlingo wathunthu (CR) wa 5% kwa odwala mankhwala osokoneza bongo, omwe ali ndi zida zambiri. Kwa iwo omwe ali ndi SCCHC, ORR inali 23% ndipo chiwerengero cha CR chinali 3%. Kuphatikizidwa sikukwanitsa kusasanthula odwala omwe ali ndi khansara ya ovari ndi khansa yoipa (CRC).

"INCB024360 powder pamodzi ndi nivolumab inali yogwira ntchito m'thupi lachiwiri la melanoma ndi squamous cell carcinoma ya mitu ya mutu ndi khosi," anatero Dr. Karl D. Lewis, MD, pulofesa wothandizira, Division of Medical Oncology, University of Colorado Anschutz Medical Campus. "Ankayankhidwa ngakhale kuti PD-L1yo ndi maonekedwe a HPV analibe. Mayankho onse ankapitirira pa data cutoff. "

Mu gawo lomwe ine ndikugawana nawo phunziro, Epacadostat ufa wa mlingo wawonjezeka kuchokera ku 25 mg kawiri tsiku lililonse kwa 300 mg kawiri tsiku lililonse. Mu gawo lachiwiri, odwala amalandira 100 mg kawiri tsiku ndi tsiku ndi 300 mg kawiri tsiku lililonse la Epacadostat powder. Nivolumab poyamba ankagwiritsidwa ntchito pa 3 mg / kg ma sabata onse a 2, omwe anasinthidwa ku 240 mg IV IV masabata onse a 2 mu gawo lachiwiri la phunzirolo. Zomwe anapeza pa ASCO zokhudzana ndi chitetezo zinachokera ku mbali zonse za phunziroli pamene zotsatira zowona bwino zinali kuchokera ku gulu lachiwiri lachiwiri.

Kwa odwala matenda a khansa yosatetezedwa (N = 40), ORR ndi mlingo wa 100-mg (n = 6) wa INCB024360 ufa ndi 100%, yomwe inali ndi mayankho a mbali zonse. Ndi chiwerengero cha 300-mg (n = 34), ORR inali 56% ndipo chiwerengero cha CR chinali 6%. Kuyeza kwa matenda (DCR; ORR kuphatikizapo matenda osalimba) anali 85%. Kwa iwo okhala ndi zotupa za PD-L1-positive (n = 7), ORR inali 71% poyerekeza ndi 29% mu gulu la PD-L1 (n = 7). Mayankho onse anali opitirira, ndi nthawi yamkati ya masabata a 16 +.

Mu gulu la SCCHN, limene odwala analandira mayendedwe oyamba a ≤2, ORR ndi 100-mg mlingo (n = 7) wa Epacadostat ufa unali 14%, panalibe CR, ndipo DCR inali 61%. Mu mkono wa 300-mg (n = 24), ORR inali 25%, ndi 1 CR ndi DCR ya 71%. Odwala omwe ali ndi tumimba za PD-L1 (n = 10) anali ndi ORR ya 30% ndipo omwe ali ndi zotupa zoipa (n = 8) anali ndi ORR ya 13%. Mayankho onse anali kupitilira pa kusanthula, ndi masabata apakati kuposa 24 + milungu.

Mu 29 odwala odwala khansa ya ovari, ORR anali 14% ndipo DCR inali 31%. Panali 1 CR mwa wodwalayo yemwe anali ndi mankhwala osadziwika, matenda a BRCA-negative, PD-L1-positive. Mu odwala 26 ali ndi CRC, omwe ali ndi vuto la microsatellite (MSI) anali ndi ORR ya 25% ndipo awo omwe anali ndi matenda osakanikirana ndi microsatellite sanayankhe.

"INCB024360 powder pamodzi ndi nivolumab sanasonyeze chizindikiro chothandiza kwa anthu osasamala omwe ali ndi khansa ya ovari ndi odwala CRC," Lewis adanena za zotsatira. Ponena za kafukufuku wam'tsogolo, adanena kuti "zotsatira zoyambirira zoteteza chitetezo ndi zothandiza zimapitiriza kufufuza za nivolumab ndi Epacadostat powder odwala omwe ali ndi matenda a khansa ya khansa komanso odwala omwe ali ndi SCCHN."

Nkhuku Yaikulu ya Epacadost

10grams yayamba.
Funso labwino kwambiri (mkati mwa 1kg) lingatumizedwe mu maola a 12 mutatha kulipira.
Kuti mukhale wamkulu (mkati mwa 1kg) mukhoza kutumizidwa mu tsiku la ntchito 3 mutatha kulipira.

Kampani Yogulitsa Yowonjezera INCB024360

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Epacadostat (INCB024360) powder (1204669-58-8) hplc =98% | AASraw

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