Nirmatrelvir
Nirmatrelvir ke inhibitor ea SARS-CoV-2 main protease (Mpro), eo hape e bitsoang 3C-like protease (3CLpro) kapa nsp5 protease. Thibelo ea SARS-CoV-2 Mpro e etsa hore e se khone ho sebetsana le li-precursors tsa polyprotein, ho thibela ho ikatisa ha vaerase.
Nirmatrelvir e thibetse ts'ebetso ea recombinant SARS-CoV-2 Mpro tekong ea biochemical ea likhakanyo tse ka fihlellehang ka vivo. Nirmatrelvir e ile ea fumanoa e tlama ka kotloloho sebakeng se sebetsang sa SARS-CoV-2 Mpro ka X-ray crystallography.
Ritonavir ke HIV-1 protease inhibitor empa ha e sebetse khahlano le SARS-CoV-2 Mpro. Ritonavir e thibela CYP3A-mediated metabolism ea nirmatrelvir, e leng se bakang keketseho ea plasma ea nirmatrelvir.
Setlhare sena se khothaletsoa. E fanoe ka tumello ea ts'ebeliso ea tšohanyetso ke FDA bakeng sa kalafo ea lefu la coronavirus le bobebe ho isa ho le leka-lekaneng (COVID-19) ho batho ba baholo le bakuli ba bana (ba lilemo li 12 ho ea holimo ba boima ba lik'hilograma tse 40 kapa liponto tse 88) liphetho tse ntle tsa tlhahlobo e tobileng ea SARS-CoV-2, le ba kotsing e kholo ea ho fetela ho COVID-19 e matla, ho kenyeletsoa ho kena sepetlele kapa lefu. Nirmatrelvir/ritonavir e lokela ho qalisoa kapele kamoo ho ka khonehang ka mor'a tlhahlobo ea COVID-19 le nakong ea matsatsi a mahlano ho tloha ha matšoao a qala.
Litlhahiso li thehiloe ho EPIC-HR, teko ea Phase2/3 ea taolo ea kliniki e sa reroang e hlahlobang katleho ea nirmaltrelivir/ritonavir vs. batho ba kotsing ea ho fetela ho lefu le matla ba fokotsa menyetla ea ho kena sepetlele kapa lefu ka matsatsi a 28 ka ho 88%.
Tlhahiso18Merero ea Tlhahlobo ea Boleng e amohetsoeng4, le6merero e tlas'a tumello.
Sistimi e tsoetseng pele ea taolo ea boleng ba machabeng e ralile motheo o tiileng oa thekiso.
Tlhokomelo ea boleng e tsamaisana le potoloho eohle ea bophelo ba sehlahisoa ho netefatsa boleng le phello ea kalafo.
Sehlopha sa Litaba tsa Taolo ea Setsebi se tšehetsa litlhoko tsa boleng nakong ea kopo le ngoliso.