Lithethefatsi tse nyenyane tsa molek'hule esale e le tšiea ea indasteri ea meriana!

 NEWS    |      2024-05-21

Lithethefatsi tse nyenyane tsa molek'hule esale e le tšiea ea indasteri ea meriana!

Hoo e ka bang lilemo tse lekholo, meriana e nyenyane ea molek'hule e bile mokokotlo oa indasteri ea meriana.


Ba na le melemo ea bohlokoa tlhahisong, lipalangong le polokelong, ho latela mokuli, sepheo se fumanehang, ho itšireletsa mafung, 'me ba tsoela pele ho phetha karolo ea bohlokoa kalafong ea bakuli.


Tsoelo-pele ea theknoloji ea lilemong tse leshome tse fetileng e nolofalelitse lik'hamphani tsa meriana ho fumana le ho nts'etsapele liphekolo tse ngata tse ncha tsa limolek'hule bakeng sa ho alafa matšoao a fapaneng, 'me nakong e tlang, limolek'hule tse nyane li tla tsoelapele ho ba mots'eare oa litlhare tsa kalafo ea bongaka, ho bapaloa. karolo ea bohlokoa kalafong ea mefuta e fapaneng ea mafu.

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

Sethethefatsi se senyenyane sa molek'hule ke eng?

Lithethefatsi tse nyane tsa molek'hule li hlalosoa e le motsoako ofe kapa ofe o tlase oa boima ba limolek'hule o sibolloang, o etselitsoeng le ho ntlafatsoa ho kenella lits'ebetsong tse itseng tsa 'mele ka har'a sebōpuoa. Lithethefatsi tse tloaelehileng tsa molek'hule tse nyane li kenyelletsa lithibela-mafu (joalo ka penicillin), li-analgesics (joalo ka paracetamol), le lihomone tsa maiketsetso (joalo ka corticosteroids).

Lithethefatsi tsa limolek'hule tse nyane ke mefuta e amohetsoeng ka ho fetesisa ea lithethefatsi ho fihlela joale, e nang le bokhoni ba ho kenella ka potlako liseleng le ho sebelisana hantle le liphofu tse itseng ka har'a lisele.


Limolek'hule tse nyenyane li ka baka mekhoa ea phekolo 'meleng oa motho ka litsela tse sa tšoaneng. Mefuta e meraro e tsebahalang haholo ke:


Li-enzyme inhibitors: Limolek'hule tse nyenyane li kena-kenana le tsoelo-pele ea mafu ka ho thibela tšebetso ea li-enzyme;


• Li-agonists / bahanyetsi ba amohelang: Limolek'hule tse nyenyane li sebelisana le liprotheine tse teng ka holim'a sele ho kenya kapa ho thibela li-receptors;


Li-modulators tsa Ion: Lithethefatsi tse nyane tsa molek'hule li ka laola ho buloa le ho koaloa ha likanale tsa ion ho laola ho kena le ho tsoa ha li-ion le ho alafa mafu a kang lefu la sethoathoa.


Mekhoa ena ea ts'ebetso kaofela e kenyelletsa sebaka se itseng sa protheine, e leng mokotla o tlamang kapa sebaka se sebetsang sa limolek'hule tse nyane. Nts'etsopele ea limolek'hule tse nyane hangata li thehiloe mohopolong oa khale oa senotlolo sa senotlolo, o ikamahanyang le moralo oa limolek'hule tse nyane tse ipapisitseng le sebaka, hydrophobicity, le thepa ea motlakase ea pokotho e tlamang, e le ho tlama sepheo le ho ama ts'ebetso ea eona ka nepo.

Melemo ea lithethefatsi tse nyenyane tsa molek'hule


Ka ho phahama ha mefuta ea litlhare tse hlahang joalo ka li-antibodies, gene therapy, le cell therapy, litlhare tse nyane tsa molek'hule li kile tsa nkuoa li siiloe ke nako, empa ha e le hantle, litlhare tse nyane tsa molek'hule li ntse li na le ho se khonehe ha tsona.

Ha ho bapisoa le li-agent tsa likokoana-hloko, limolek'hule tse nyenyane li ntse li e-na le melemo e mengata tlhahisong, lipalangoang, ho latela mokuli, mefuta e fumanehang ea sepheo, immunogenicity, le likarolo tse ling.


Limolek'hule tse nyenyane li na le mehaho e batlang e le bonolo, e nang le boima ba molek'hule ka kakaretso e sa feteng 500 Daltons, 'me e ka etsoa ka mokhoa o ikhethileng ho finyella litlhoko tse khethehileng tsa phekolo;


Hangata e tsitsitse haholo mme ha se hangata e hlokang maemo a khethehileng a polokelo a kang ho behoa tlas'a maemo a tlaase a mocheso; Boitšoaro 'meleng hangata bo ka lebelloa esale pele ebile ho bonolo ho bo laola.


Ntle le moo, limolek'hule tse nyane li ka potoloha le ho tsamaea ka har'a 'mele, tsa fetisoa ho tloha ka mpeng ka phallo ea mali ho ea sebakeng sa ts'ebetso, tsa kenella ka har'a membrane ea sele ho fihlela sepheo sa intracellular, 'me li na le ts'ebetso e ngata e ngata, e etsang hore e be ea bohlokoa haholo mafapheng a fapaneng a bongaka joalo ka. oncology, bophelo bo botle ba pelo, mafu a tšoaetsanoang, bophelo bo botle ba kelello le mafu a methapo ea kutlo.

Limolek'hule tse nyane li bile teng, li, 'me li tla tsoelapele ho ba tsona tse ka sehloohong tsa meriana ea kalafo nakong e fetileng, ea hajoale le e tlang.

Lilemong tse 15 ho isa ho tse 20 tse fetileng, palo e kholo ea lithethefatsi tsa molek'hule e amohetsoe ke FDA mme e bile le tšusumetso e kholo tlhokomelong ea bakuli, ho kenyelletsa Cymbalta bakeng sa ho phekola khatello ea maikutlo le matšoenyeho, Viagra bakeng sa ho phekola ho se sebetse ha erectile, Tagrisso bakeng sa ho lebisa tlhokomelo ea NSCLC, le Eliquis bakeng sa fibrillation ea atrial le anticoagulation.


Ebile, palo ea litlhare tse ncha tsa limolek'hule tse amohetsoeng ke FDA e eketsehile ka 50% selemong se fetileng, ka litlhare tse 34 tse ncha tsa molek'hule tse amohetsoeng ka 2023 mme tse 21 feela ka 2022. Kakaretso ea FDA e amohetse lithethefatsi tse ncha ka 2023, e bonts'ang hore limolek'hule tse nyane li ntse li le bohlokoa bakeng sa nts'etsopele ea tlhokomelo ea bophelo bo botle.


Lethathamong le holimo la 100 la thekiso ea lithethefatsi ka 2021, ho bile le kakaretso ea limolek'hule tse nyane tse 45 tsa lithethefatsi, tse etsang 36% ea kakaretso ea chelete ea thekiso; Ho na le lithethefatsi tse 11 tse nyane tsa molek'hule tse thibelang hlahala tse kentseng lethathamong la TOP100, ka kakaretso ea chelete ea thekiso ea lidolara tse limilione tse likete tse 51.901 tsa US. Chelete e phahameng ka ho fetisisa ea thekiso ke lidolara tse limilione tse likete tse 12.891 tsa US bakeng sa lenalidomide; Ka 2022, thekiso e felletseng ea litlhare tse nyane tsa molek'hule ho Top 10 feela e fihlile ho lidolara tse limilione tse likete tse 96.6, ha Paxlovid a rekisa ho fihla ho lidolara tse libilione tse 18.9 lefatšeng ka bophara, a bonts'a ka botlalo bokhoni ba 'maraka ba lithethefatsi tsa molek'hule.