I-Tofacitinib citrate yiyeza elimiselweyo (igama lokurhweba i-Xeljanz) elaphuhliswa ekuqaleni nguPfizer kwiklasi ye-oral Janus kinase (JAK) inhibitors. Inokuthintela ngokukhethekileyo i-JAK kinase, ibhloke iindlela ze-JAK / STAT, kwaye ngaloo ndlela inqanda ukuhanjiswa kwesignali yeseli kunye ne-Related gene expression kunye nokusebenza, esetyenziselwa ukunyanga i-rheumatoid arthritis, i-psoriatic arthritis, i-ulcerative colitis kunye nezinye izifo ze-immune.

Ichiza libandakanya iifom ezintathu zedosi: iipilisi, iipilisi ezikhutshwa ngokuqhubekayo kunye nezisombululo zomlomo. Iipilisi zayo zaqala ukuvunywa yi-FDA kwi-2012, kwaye ifom yedosi yokukhutshwa ngokuqhubekayo yavunywa yi-FDA ngoFebruwari 2016. Iyokuqala ukunyanga amalunga e-rheumatoid. I-Yan yi-JAK inhibitor ethathwe ngomlomo kanye ngosuku. NgoDisemba ka-2019, isalathiso esitsha samachiza akhutshwa ngokuzinzileyo savunywa kwakhona ukuba aphakathi ukuya kwi-UC. Ukongezelela, izilingo zekliniki zesigaba se-3 se-plaque psoriasis sele zigqityiwe, kwaye ezinye iimvavanyo zekliniki ze-3 ziyaqhubeka, ezibandakanya i-psoriatic arthritis esebenzayo, i-juvenile idiopathic arthritis, njl. Uhlobo lwezibonakaliso. Izibonelelo zeepilisi ezikhutshwa ngokuzinzileyo ezithatha ixesha elide kwaye zifuna ukuba zithathwe kanye kuphela ngosuku ziluncedo kulawulo nolawulo lwezifo zezigulane.

Ukusukela ekudwelisweni kwayo, iintengiso zayo ziye zanda unyaka nonyaka, zafikelela kwi-2.242 yeebhiliyoni zeedola zaseMelika ngo-2019. E-China, ifom yedosi yethebhulethi yamkelwa ukuba ithengiswe ngoMatshi ka-2017, kwaye yangena kwikhathalogu ye-inshurensi yezonyango ngothethwano ngo-2019. ibhidi yi-RMB 26.79. Nangona kunjalo, ngenxa yemiqobo ephezulu yobugcisa yamalungiselelo okukhululwa okuzinzileyo, le fomu yedosi ayikathengiswa e-China.

I-JAK kinase idlala indima ebalulekileyo ekudumbeni, kwaye i-inhibitors yayo ibonakaliswe ukunyanga izifo ezithile ezivuthayo kunye ne-autoimmune. Ukuza kuthi ga ngoku, i-7 JAK inhibitors ivunyiwe kwihlabathi jikelele, kuquka i-Leo Pharma's Delgocitinib, i-Celgene's Fedratinib, i-AbbVie's upatinib, i-Astellas's Pefitinib, i-Eli Lilly's Baritinib kunye ne-Novartis's Rocotinib. Nangona kunjalo, kuphela i-tofacitinib, i-baritinib kunye ne-rocotinib evunyiweyo e-China phakathi kweziyobisi ezikhankanywe ngasentla. Sijonge ngamehlo abomvu “iTofatib Citrate Sustained Release Release” zikaQilu zivunywe ngokukhawuleza kwaye kuxhamle izigulane ezininzi.

E-China, uphando lwangaphambili lwe-tofacitib citrate luvunyiwe yi-NMPA ngo-Matshi 2017 kunyango lwezigulane ze-RA zabantu abadala abangasebenzi ngokwaneleyo okanye ukunganyamezeli kwi-methotrexate, phantsi kwegama lezorhwebo elithi Shangjie. Ngokwedatha evela kuMeinenet, ukuthengiswa kweetafile ze-tofacitib citrate kumaziko ezonyango aseTshayina ngo-2018 zazizizigidi ezisisi-8.34 zeeyuan, ezaziphantsi kakhulu kunentengiso yayo yehlabathi. Inxalenye enkulu yesizathu lixabiso. Kuxelwe ukuba ixabiso lokuqala lika-Shangjie lokuthengisa laliyi-2085 yuan (5mg*28 tablets), kwaye iindleko zenyanga zaziyi-4170 yuan, ayingomthwalo omncinci kwiintsapho eziqhelekileyo.

Nangona kunjalo, kuyafaneleka ukubhiyozela ukuba i-tofacitib ifakwe kwi-2019 "I-Inshurensi yeSizwe yezoNyango, i-Inshurensi yokulimala komsebenzi kunye noLuhlu lweziyobisi ze-Inshurensi ye-Maternity" yi-National Medical Insurance Administration emva kothethathethwano ngoNovemba 2019. Kuxelwa ukuba umrhumo wenyanga uya kuncitshiswa. ukuya ngaphantsi kwama-2,000 eyuan emva kokuba kuxoxiwe ukuthotywa kwexabiso, okuya kuphucula kakhulu ukufumaneka kwechiza.

Ngo-Agasti ka-2018, iBhodi yokuHlola kwakhona i-Patent ye-ofisi ye-State Intellectual Property yenze isigqibo sokuphonononga isicelo se-36902 sokungasebenzi, kwaye yabhengeza ukuba ayisebenzi i-patent engundoqo ye-Pfizertofatib, i-compound patent, ngenxa yezizathu zokungachazwa ngokwaneleyo kwenkcazo. Nangona kunjalo, i-patent ye-Pfizertofatiib crystal form (ZL02823587.8, CN1325498C, umhla wesicelo 2002.11.25) iya kuphelelwa yisikhathi kwi-2022.

I-database ye-Insight ibonisa ukuba, ukongeza kuphando lokuqala, amachiza amahlanu enziwe afana nalawo enziwe afana nalawo enziwe afana nalawo enziwe afana nalawo enziwe afana nalawo eChia Tai Tianqing, iQilu, iKelun, iYangtze River, kunye neNanjing Chia Tai Tianqing avunyiwe ukuba athengiswe kuqulunqo lwethebhulethi yetofacitinib yasekhaya. Nangona kunjalo, kuhlobo lwethebhulethi yokukhutshwa ngokuzinzileyo, kuphela uphando lwangaphambili lwePfizer olungenise isicelo sokuthengisa ngoMeyi 26. I-Qilu yinkampani yokuqala yasekhaya ukungenisa isicelo sokuthengisa kolu qulunqo. Ukongeza, i-CSPC Ouyi ikwinqanaba lovavanyo lwe-BE.

I-Changzhou Pharmaceutical Factory (CPF) ngumvelisi ohamba phambili wamachiza we-APIs, uqulunqo olugqityiweyo e-China, oluse-Changzhou, kwiphondo laseJiangsu. I-CPF isekelwe kwi-1949. Sizinikezele kwi-Tofacitinib Citrate ukusuka kwi-2013, kwaye singenise i-DMF kakade. Sibhalise kumazwe amaninzi, kwaye sinokukuxhasa ngenkxaso yamaxwebhu angcono eTofacitinib Citrate.