ABCB1 limits brain exposure of the KRAS<sup>G12C</sup> inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability.

Loos, Nancy H C; Retmana, Irene A; Li, Wenlong; Martins, Margarida L F; Lebre, Maria C; Sparidans, Rolf W; Beijnen, Jos H; Schinkel, Alfred H

ABCB1 limits brain exposure of the KRAS^G12C inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability.

Loos, Nancy H C; Retmana, Irene A; Li, Wenlong; Martins, Margarida L F; Lebre, Maria C; Sparidans, Rolf W; Beijnen, Jos H; Schinkel, Alfred H.

Afiliação

Loos NHC; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands.
Retmana IA; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands; Utrecht University, Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmacology, Utrecht, The Netherlands.
Li W; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands.
Martins MLF; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands.
Lebre MC; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands.
Sparidans RW; Utrecht University, Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmacology, Utrecht, The Netherlands.
Beijnen JH; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands; Utrecht University, Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmacoepidemiology and Clinical Pharmacology, Utrecht, The Netherlands; The Netherlands Cancer Institute, Division of P
Schinkel AH; The Netherlands Cancer Institute, Division of Pharmacology, Amsterdam, The Netherlands. Electronic address: a.schinkel@nki.nl.

Pharmacol Res ; 178: 106137, 2022 04.

Article em En | MEDLINE | ID: mdl-35192958

Assuntos

Carcinoma Pulmonar de Células não Pequenas; Neoplasias Pulmonares; Subfamília B de Transportador de Cassetes de Ligação de ATP/genética; Animais; Disponibilidade Biológica; Encéfalo/metabolismo; Citocromo P-450 CYP3A/genética; Citocromo P-450 CYP3A/metabolismo; Cães; Humanos; Células Madin Darby de Rim Canino; Camundongos; Camundongos Knockout; Piperazinas; Proteínas Proto-Oncogênicas p21(ras); Piridinas; Pirimidinas

Palavras-chave

10322450); 137278711); ABCB1/P-glycoprotein; ABCG2/Breast cancer resistance protein; Cytochrome P450 3A; Elacridar HCl (PubChem CID: 170320); KRAS(G12C) inhibitor; Ko143 (PubChem CID; Pharmacokinetics; Sotorasib; Sotorasib (PubChem CID; Zosuquidar (PubChem CID: 153997)

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Carcinoma Pulmonar de Células não Pequenas / Neoplasias Pulmonares Idioma: En Ano de publicação: 2022 Tipo de documento: Article

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