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An open-label, phase 1, randomized, three treatments, three-period, crossover, relative bioavailability study of CC-292, a potent and orally available inhibitor of bruton tyrosine kinase.
Cheng, Yiming; Liu, Liangang; Xue, Yongjun; Zhou, Simon; Li, Yan.
Afiliação
  • Cheng Y; Clinical Pharmacology & Pharmacometrics, Bristol Myers Squibb, Summit, New Jersey, USA.
  • Liu L; Global Biometrics and Data Sciences, Bristol Myers Squibb, Berkeley Heights, New Jersey, USA.
  • Xue Y; Non-Clinical Research & Development, Bristol Myers Squibb, Summit, New Jersey, USA.
  • Zhou S; Clinical Pharmacology & Pharmacometrics, Bristol Myers Squibb, Summit, New Jersey, USA.
  • Li Y; Clinical Pharmacology & Pharmacometrics, Bristol Myers Squibb, Summit, New Jersey, USA.
J Clin Pharm Ther ; 47(8): 1186-1193, 2022 Aug.
Article em En | MEDLINE | ID: mdl-35307850
WHAT IS KNOWN AND OBJECTIVE: CC-292 is a potent, selective, orally administered small molecule inhibitor of bruton tyrosine kinase (BTK). The aim of this study was to evaluate the relative bioavailability of newly developed CC-292 tablet formulation (P22 tablet (P22-TAB) and CC-292 capsule formulation (P22 capsule [P22-CAP]) compared to the current CC-292 capsule formulation (P1 capsule [P01-CAP]). METHODS: This was an open-label, randomized, three-period, crossover study in healthy subjects (N = 12). Blood samples for pharmacokinetics (PK) assessment were collected up to 48 h postdose during each treatment period. Safety was evaluated throughout the study. RESULTS AND DISCUSSION: For all three formulations, following administration of CC-292 at a dose level of 250 mg under fasted conditions, CC-292 was rapidly absorbed with maximum plasma concentrations (Cmax) occurring at a median of 1.5-1.75 h (Tmax). P22-CAP formulation showed a similar range of Tmax compared to P01-CAP and P22-TAB showed a wider range of Tmax compared to P01-CAP. Comparable or higher Cmax and AUC0-∞ were noted for P22-TAB and P22-CAP formulations as compared to P01-CAP formulation. The relative bioavailability (Frel) of the CC-292 P22-TAB compared to the P01-CAP reference formulation was 1.02, and the relative bioavailability (Frel) of the CC-292 P22-CAP compared to the P01-CAP reference formulation was 1.23. In conclusion, CC-292 was well tolerated when administered as single 250-mg oral doses of P22-TAB, P22-CAP or P01-CAP in the fasted state in this group of healthy subjects. Given that CC-292 has shown favourable safety profiles in the current clinical settings, the new formulations (P22-TAB and P22-CAP) are similar as the reference formulation (P01-CAP).
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Disponibilidade Biológica Tipo de estudo: Clinical_trials / Prognostic_studies Limite: Humans Idioma: En Revista: J Clin Pharm Ther Assunto da revista: FARMACIA / TERAPEUTICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Disponibilidade Biológica Tipo de estudo: Clinical_trials / Prognostic_studies Limite: Humans Idioma: En Revista: J Clin Pharm Ther Assunto da revista: FARMACIA / TERAPEUTICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Reino Unido