New designs for HIV-1 integrase inhibitors: a patent review (2018-present).
Expert Opin Ther Pat
; 33(1): 51-66, 2023 Jan.
Article
en En
| MEDLINE
| ID: mdl-36750766
ABSTRACT
INTRODUCTION:
Combination antiretroviral therapy (cART) has dramatically reduced morbidity and mortality of HIV-1-infected patients. Integrase strand transfer inhibitors (INSTIs) play an important role as a key drug in cART. The second-generation INSTIs are very potent, but due to the emergence of highly resistant viruses and the demand for more conveniently usable drugs, the development of 'third-generation' INSTIs and mechanistically different inhibitors is actively being pursued. AREAS COVERED This article reviews the patents (from 2018 to the present) for two classes of HIV-1 integrase inhibitors of INSTIs and integrase-LEDGF/p75 allosteric inhibitors (INLAIs). EXPERT OPINION Since the approval of the second-generation INSTI dolutegravir, the design of new INSTIs has been mostly focused on its scaffold, carbamoylpyridone (CAP). This CAP scaffold is used not only for HIV-1 INSTIs but also for drug discoveries targeting other viral enzymes. With the approval of cabotegravir as a regimen of long-acting injection in combination with rilpivirine, there is a growing need for longer-acting agents. INLAIs have been intensely studied by many groups but have yet to reach the market. However, INLAIs have recently been reported to also function as a latency promoting agent (LPA), indicating further development possibilities.Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Infecciones por VIH
/
VIH-1
/
Inhibidores de Integrasa VIH
/
Integrasa de VIH
/
Fármacos Anti-VIH
Límite:
Humans
Idioma:
En
Revista:
Expert Opin Ther Pat
Asunto de la revista:
TERAPEUTICA
Año:
2023
Tipo del documento:
Article
País de afiliación:
Japón