Cetilistat phofo ke lithethefatsi tse etselitsoeng ho phekola botenya. E sebetsa ka tsela e ts'oanang le orchidat ea khale ea lithethefatsi (Xenical) ka ho thibela pancreatic lipase, enzyme e robehang triglycerides ka mpeng. Ntle le enzyme ena, li-triglycerides tse tsoang lijong li thibetsoe ho ba li-hydrolyzed ka meharo ea mahala ea mafura 'me ha li sa fuoe ntle le ho feta. Cetilistat e ile ea bontšoa ho hlahisa tahlehelo e tšoanang ea boima ba 'mele ho orlistat.
lebitso | Peso ea Cetilistat |
CAS | 282526-98-1 |
Ho hloeka | 98.0% (HPLC) |
Lebitso la k'hemik'hale | 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one |
Li-synonyms | Cetilistat 282526-98-1 Litlhaku EA-962 EA-962 |
Molecular Formula | C25H39NO3 |
Boima ba 'mele | 401.591 g / mol |
Melting Point | 74-76 ° C |
InChI Key | MVCQKIKWYUURMU-UHFFFAOYSA-N |
foromo | tiileng |
Ponahalo | White ho Off-White Powder |
Halofo ea bophelo | Half-life of 9.4-16 h ho batho, e telele ho feta ea likhoto (4.4 h) le lintja tse fepehileng (7.3 h) |
Solubility | Chloroform (Slighlty), Ethyl Acetate (Hanyane) |
Boemo Storage | Sehatsetsi |
kopo | E batloa bakeng sa ts'ebeliso / kalafo ho botenya. |
Tokomane ea Teko | fumaneha |
Ho nona haholo ke seoa sa sejoale-joale linaheng tse tsoetseng pele le tse tsoelang pele moruong, 'me ha joale boima ba' mele le botenya li baka lefu le fetang lefats'e ho feta boima. Cetilistat ke rialo, e sebetsang ka molomo, ea ka mpeng le ea pancreatic lipase inhibitor. Lithutong tsa in vitro cetilistat inhibited lipancreatic lipase ea motho ea nang le IC50 e maemong a tlaase a nanomolar. Karolong ea Bobeli likokoana-hloko tsa bakuli ba batenya le ho bakuli ba batenya haholo ba nang le lefu la tsoekere la 2, cetilistat e tsamaisoang libeke tse 12 e fokolitse boima ba 'mele haholo, serum low-density lipoprotein (LDL) cholesterol le cholesterol e felletseng ka ho bapisoa le placebo. Karolo ea bakuli ba batenya ho feta tekano ba fihletseng phokotso ea boima ba 'mele ea bonyane 5% e ne e le kholo ho matsoho ohle a sebetsang ha ho bapisoa le placebo. Ho bakuli ba nang le lefu la tsoekere le lengata maemo a "glycosylated hemoglobin" (HbA1c) le ona a fokotsehile haholo. Cetilistat e bontšitse bonolo ho liketsahalo tse mpe tse leka-lekaneng, boholo ba tlhaho ea sefuba (steatorrhea), e nang le ketsahalo e tlase ho feta ea orlistat. E sa tsoa amoheloa Japane bakeng sa kalafo ea botena le mathata.
E ntlafalitsoe ke Alizyme, k'hamphani e ikhethang ea biopharmaceutical ka tšebelisano le Takeda Pharmaceutical, cetilistat (ATL-962) ke kalafo ea liteko bakeng sa botena. Cetilistat e thibela lipase tsa pancreatic mme e sebetsa e le moemeli ho phekola botenya le lefu la tsoekere le amanang le eona.
E fella ka boima ba 'mele mme e monya mafura lijong. Setlhare se sebetsa ka hohle-hohle ho fokotsa takatso ea lijo, ntle le ho ama bokong.
Ka December 2008, Takeda o ile a qala thuto ea bongaka ea Phase III ea cetilistat Japane. Tswelopele ea liteko tsa mantlha tsa karolo ea bohlano ea mantlha e ile ea latela tlhaiso-leseling ea tlhahlobo ea bongaka ea Phase II e bonts'ang cetilistat e khothalelitse ho fokotsa boima ba 'mele mme ka kakaretso e ne e mamelloa ho bakuli ba batenya haholo.
Takeda o ile a lekola datha ea European II ea cetilistat ka Phato 2003 mme ka Pherekhong 2004 a etsa tumellano le Alizyme ea ho nts'etsapele, ho etsa le ho rekisa cetilistat Japane.
Ka Mphalane 2012, Takeda o ile a kenya Kopo e Ncha ea Kopano ea Lithethefatsi (NDA) bakeng sa Cetilistat ho Lekala la Bophelo la Lefapha la Bophelo, Basebetsi le Boiketlo ba Sechaba bakeng sa kalafo ea botenya.
Patlisiso le nts'etsopele ea hajoale ea Alizyme e shebane le kalafo ea mafu a ka mpeng, botena, kankere le lefu la tsoekere.
Cetilistat ke gastrointestinal lipase inhibitor e thibelang ho hlohlona ha mafura le ho monya, e lebisang ho phokotsong ea matla, ka hona ho fokotsa boima ba 'mele. E khethollotse ho li-ejenti tse ling tse khahlanong le botenya hobane e sa sebetse bokong ho fokotsa takatso ea lijo, empa e sebetsa ka mokhoa o sa lekanyetsoang. K'hemik'hale e lula e le ka mpeng ea mpa ea mpa e se na letho le kenang 'meleng.
Cetilistat, tlasa lebitso la brand Cetislim, Checkwt, kapa Kilfat, ke setlhare se secha se ntseng se etsoa liteko le tsa bongaka likarolong tse fapaneng tsa lefats'e ka katleho ea sona.
Cetilistat e thathamisitsoe tlas'a sehlopha sa "lithibela-mafu tse khahlanong le botenya kapa lithethefatsi". Ho nona ke e 'ngoe ea mathata a bohlokoa a mehleng ea kajeno, haholoholo linaheng tse tsoelang pele le tse tsoetseng pele.
Cetilistat ke lithethefatsi tse khahlanong le botenya tse kenang kahare. E sebetsa haholo e le gastrointestinal le pancreatic lipase inhibitor.
Cetilistat e sebelisoa e le tlatsetso ea lijo tse phetseng hantle le boikoetliso bakeng sa nako e khuts'oane kalafong ea botenya. Cetilistat e boetse e sebelisetsoa merero e sa fumaneheng ho tataiso ea meriana.
Cetilistat ke lithethefatsi tse thibelang botenya mme hona joale li ntse li etsoa lipatlisiso Japane, US le Europe. Hobane Cetilistat e ntse e feta litekong tsa bongaka, ha ho na ts'ebetso kapa polokeho e netefalitsoeng e sa le moriana ona.
Litekong tsa batho, cetilistat e bonts'itsoe ho hlahisa tahlehelo e tšoanang ea boima ba 'mele ho orlistat, empa e boetse e hlahisa litla-morao tse tšoanang le mafura, litulo tse hlephileng, ho theoha ha mokokotlo, ho sisinyeha ha methapo hangata le ho bata. Ho ka etsahala hore ho ka ba le lithibelo tse tšoanang ho ts'oaroeng ha vithamine e qhibilihang ka mafura le limatlafatsi tse ling tse nang le mafura hore li se ke tsa haella.
Cetilistat e phethetse liteko tsa Karolo ea 1 le ea 2 Bophirima 'me hajoale e litekong tsa Phase 3 Japane moo e kopaneng le Takeda. Norgina BV joale e fumane litokelo tse felletseng tsa lefats'e tsa cetilistat ho tsoa Alizyme kamora hore e qale ho kena tšebetsong.
Teko ea bobeli e phatlalalitsoeng e fumane cetilistat e theotse boima ba 'mele haholo mme e mamelletsoe hamolemo ho feta orlistat.