Izidakamizwa ezincane ze-molecule bezilokhu ziyinsika yemboni yezokwelapha!

 NEWS    |      2024-05-21

Izidakamizwa ezincane ze-molecule bezilokhu ziyinsika yemboni yezokwelapha!

Cishe ikhulu leminyaka, izidakamizwa ezincane ze-molecule beziwumgogodla wemboni yezokwelapha.


Banezinzuzo ezibalulekile ekukhiqizeni, kwezokuthutha nasekugcineni, ukuthobela isiguli, ububanzi obuhlosiwe obutholakalayo, ukuzivikela komzimba, futhi bayaqhubeka nokubamba iqhaza elibalulekile ekwelashweni kwesiguli.


Ukuthuthuka kwezobuchwepheshe kule minyaka eyishumi edlule kwenze izinkampani zemithi zithole futhi zithuthukise izindlela zokwelapha zamangqamuzana amancane kakhulu ezokwelapha izinkomba ezahlukahlukene, futhi ngokuzayo, ama-molecule amancane azoqhubeka nokuba yisisekelo semithi yokwelapha, edlala i-athomu. indima ebalulekile ekwelapheni uhla lwezifo.

Small molecule drugs have always been the pillar of the pharmaceutical industry!

Uyini umuthi we-molecule encane?

Izidakamizwa ze-molecule encane zichazwa njenganoma iyiphi inhlanganisela ye-organic yesisindo esiphansi etholakala, eklanyelwe, futhi yathuthukiswa ukungenelela ezinqubweni ezithile zomzimba ngaphakathi kwento ephilayo. Izidakamizwa ezivamile ze-molecule ezincane zihlanganisa ama-antibiotics (njenge-penicillin), ama-analgesics (afana ne-paracetamol), namahomoni okwenziwa (njenge-corticosteroids).

Izidakamizwa ze-molecule encane ziyizinhlobo zezidakamizwa ezigunyazwe kakhulu kuze kube manje, ezinekhono lokungena ngokushesha kulwelwesi lwamaseli futhi luhlanganyele ngokunembile nokuhlosiwe okuqondile ngaphakathi kwamaseli.


Ama-molecule amancane angabangela ukusabela kokwelapha emzimbeni womuntu ngezindlela ezihlukahlukene. Izinhlobo ezintathu ezivame kakhulu yilezi:


Ama-Enzyme inhibitors: Ama-molecule amancane angenela ekuqhubekeleni phambili kwesifo ngokuvimbela umsebenzi we-enzyme;


• Ama-agonists/abaphikisi abamukelayo: Ama-molecule amancane asebenzisana namaprotheni akhona endaweni yeseli ukuze asebenze noma avimbe ama-receptors;


Amamojula wesiteshi se-Ion: Izidakamizwa ze-molecule ezincane zingalawula ukuvulwa nokuvalwa kwamashaneli e-ion ukulawula ukungena nokuphuma kwama-ion futhi zelaphe izifo ezifana nesifo sokuwa.


Lezi zindlela zokwenza zonke zibandakanya indawo ethile kuphrotheni, okuyiphakethe elibophayo noma indawo esebenzayo yama-molecule amancane. Ukuthuthukiswa kwama-molecule amancane ngokuvamile kusekelwe kumbono wemodeli yokhiye wokukhiya wakudala, ovumelanisa ukwakheka kwama-molecule amancane ngokusekelwe esikhaleni, i-hydrophobicity, kanye nezakhiwo zikagesi zephakethe elibophayo, ukuze libophe ngempumelelo ithagethi futhi lithinte umsebenzi walo.

Izinzuzo zezidakamizwa ezincane ze-molecule


Ngokukhula kwamamodeli ezidakamizwa asafufusa anjengamasosha omzimba, ukwelashwa kwezakhi zofuzo, nokwelashwa kwamaseli, izidakamizwa ezincane ze-molecule zake zabhekwa njengeziphelelwe yisikhathi, kodwa empeleni, izidakamizwa ezincane ze-molecule zisenokungaphinde zisebenze.

Uma kuqhathaniswa nama-agent aphilayo, ama-molecule amancane asenezinzuzo ezibalulekile ekukhiqizeni, ezokuthutha, ukuthobela isiguli, ububanzi obuhlosiwe obutholakalayo, i-immunogenicity, nezinye izici.


Ama-molecule amancane anezakhiwo ezilula, anesisindo samangqamuzana ngokuvamile esingadluli ama-Dalton angu-500, futhi angenziwa ngokwezifiso ukuze ahlangabezane nezidingo ezithile zokwelapha;


Ivamise ukuzinza kakhulu futhi ayivamisile ukudinga izimo ezikhethekile zokuyigcina njengokubekwa ngaphansi kwezimo eziphansi zokushisa; Ukuziphatha emzimbeni kuvame ukubikezelwa futhi kulula ukukuphatha.


Ngaphezu kwalokho, ama-molecule amancane angajikeleza kalula futhi ahambe ngaphakathi komzimba, adlulise esuka emathunjini ngokugeleza kwegazi aye endaweni yesenzo, angene kulwelwesi lweseli ukuze afinyelele imigomo ye-intracellular, futhi abe nokusebenza okuningi okucebile, okuwenza abe semqoka emikhakheni ehlukahlukene yezokwelapha njenge. i-oncology, impilo yenhliziyo nemithambo yegazi, izifo ezithathelwanayo, impilo yengqondo, kanye nezifo zemizwa.

Ama-molecule amancane abelokhu, akhona, futhi azoqhubeka abe insika yemithi yokwelapha emtholampilo esikhathini esidlule, samanje, nekusasa.

Eminyakeni eyi-15 kuye kwengama-20 edlule, inani elikhulu lezidakamizwa ezincane ze-molecule zivunyelwe yi-FDA futhi zibe nomthelela omkhulu ekunakekelweni kwesiguli, okuhlanganisa i-Cymbalta yokwelapha ukucindezeleka nokukhathazeka, i-Viagra yokwelapha ukungasebenzi kahle kwe-erectile, i-Tagrisso yokukhomba i-NSCLC, kanye ne-Eliquis ye-atrial fibrillation kanye ne-anticoagulation.


Eqinisweni, inani lemithi emincane ye-molecule emisha egunyazwe i-FDA lenyuke ngaphezu kuka-50% ngonyaka odlule, nemithi engama-molecule emincane engama-34 evunywe ngo-2023 futhi engama-21 kuphela ngo-2022. Ingqikithi ye-FDA igunyaze izidakamizwa emisha ngo-2023, okukhombisa ukuthi ama-molecule amancane asabalulekile ekuthuthukisweni kokunakekelwa kwezempilo.


Ohlwini oluphezulu oluyi-100 lokuthengiswa kwezidakamizwa ngo-2021, kwakukhona isamba sezidakamizwa ezincane ezingama-molecule angu-45, ezibalelwa ku-36% wesamba semali engenayo yokuthengisa; Kunezidakamizwa eziyi-11 ezincane ezilwa nesimila ezingene ohlwini lwe-TOP100, nesamba semali engenayo yokuthengisa engama-dollar ayizigidi eziyizinkulungwane ezingama-51.901. Imali yokuthengisa ephakeme kakhulu yi-12.891 billion yamadola ase-US ye-lenalidomide; Ngo-2022, ukuthengiswa okuphelele kwezidakamizwa ezincane ze-molecule ku-Top 10 kuphela kwafinyelela amaRandi ayizigidi eziyizinkulungwane ezingama-96.6, kanti i-Paxlovid ithengisa amadola aseMelika ayizigidi eziyizinkulungwane eziyi-18.9 emhlabeni jikelele, okukhombisa ngokugcwele amandla emakethe ezidakamizwa ezincane ze-molecule.