Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state
Introduction: Imatinib mesylate is currently the first-line oral treatment for all stages of chronic myeloid leukemia (CML) and is also used in some cases of gastrointestinal stromal tumor (GIST) and acute lymphoblastic leukemia (ALL). Objective: Investigate the bioavailability of two products cont...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Instituto Nacional de Câncer (INCA)
2023-12-01
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| Series: | Revista Brasileira de Cancerologia |
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| Online Access: | https://rbc.inca.gov.br/index.php/revista/article/view/4060 |
| _version_ | 1797225698001158144 |
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| author | Carlos Eduardo Sverdloff Vinicius Marcondes Rezende Paulo Alexandre Rebelo Galvinas Guilherme Araújo Pinto Lygia Nerath Bonanato Fernando Bastos Canton Pacheco |
| author_facet | Carlos Eduardo Sverdloff Vinicius Marcondes Rezende Paulo Alexandre Rebelo Galvinas Guilherme Araújo Pinto Lygia Nerath Bonanato Fernando Bastos Canton Pacheco |
| author_sort | Carlos Eduardo Sverdloff |
| collection | DOAJ |
| description |
Introduction: Imatinib mesylate is currently the first-line oral treatment for all stages of chronic myeloid leukemia (CML) and is also used in some cases of gastrointestinal stromal tumor (GIST) and acute lymphoblastic leukemia (ALL). Objective: Investigate the bioavailability of two products containing imatinib mesylate, 100 mg coated tablet, to determine if they are bioequivalent. Method:
The study was conducted using an open-label, randomized, balanced design and the formulations were administered orally in a single dose to 48 healthy adult males, in fed state, followed by sequential blood withdraws for the next 72 hours. Forty-eight male healthy volunteers were selected to participate in the study. Test formulation from Eurofarma Laboratórios S.A. Brazil was compared to that from Novartis Biociências S.A. The comparative bioavailability of the formulations was assessed based on statistical comparisons of relevant pharmacokinetic parameters obtained from drug concentration data from collected blood samples measured using an analytical method based on high-performance liquid chromatography coupled to mass spectrometry. Results: The ratio of the geometric means between the test and the reference, with a 90% confidence interval, of pharmacokinetic parameters for Cmax was 102.26% (94.17-111.04%) and for AUC0-t was 101.24% (95.19-107.68%). Conclusion: Imatinib mesylate 100 mg (test product) from Eurofarma Laboratórios S.A. was considered bioequivalent to the reference Glivec® 100 mg manufactured by Novartis Biociências S.A, and the test product can be interchangeable with the reference, based on their pharmacokinetic performance.
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| first_indexed | 2024-03-08T23:24:58Z |
| format | Article |
| id | doaj.art-95525337f3544657826c7a45ed02895d |
| institution | Directory Open Access Journal |
| issn | 2176-9745 |
| language | English |
| last_indexed | 2024-04-24T14:13:08Z |
| publishDate | 2023-12-01 |
| publisher | Instituto Nacional de Câncer (INCA) |
| record_format | Article |
| series | Revista Brasileira de Cancerologia |
| spelling | doaj.art-95525337f3544657826c7a45ed02895d2024-04-03T08:58:00ZengInstituto Nacional de Câncer (INCA)Revista Brasileira de Cancerologia2176-97452023-12-0169410.32635/2176-9745.RBC.2023v69n4.4060Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed stateCarlos Eduardo Sverdloff0Vinicius Marcondes Rezende1Paulo Alexandre Rebelo Galvinas2Guilherme Araújo Pinto3Lygia Nerath Bonanato4Fernando Bastos Canton Pacheco5ATCgen Pesquisa e Desenvolvimento à Saúde Ltda. Campinas (SP), Brazil.ATCgen Pesquisa e Desenvolvimento à Saúde Ltda. Campinas (SP), Brazil.Magabi Pesquisas Clínicas e Farmacêuticas. Itapevi (SP), Brazil.Magabi Pesquisas Clínicas e Farmacêuticas. Itapevi (SP), Brazil.Eurofarma Laboratórios. Itapevi (SP), Brazil.Centro Avançado de Estudo e Pesquisa (Caep). Campinas (SP), Brazil. Introduction: Imatinib mesylate is currently the first-line oral treatment for all stages of chronic myeloid leukemia (CML) and is also used in some cases of gastrointestinal stromal tumor (GIST) and acute lymphoblastic leukemia (ALL). Objective: Investigate the bioavailability of two products containing imatinib mesylate, 100 mg coated tablet, to determine if they are bioequivalent. Method: The study was conducted using an open-label, randomized, balanced design and the formulations were administered orally in a single dose to 48 healthy adult males, in fed state, followed by sequential blood withdraws for the next 72 hours. Forty-eight male healthy volunteers were selected to participate in the study. Test formulation from Eurofarma Laboratórios S.A. Brazil was compared to that from Novartis Biociências S.A. The comparative bioavailability of the formulations was assessed based on statistical comparisons of relevant pharmacokinetic parameters obtained from drug concentration data from collected blood samples measured using an analytical method based on high-performance liquid chromatography coupled to mass spectrometry. Results: The ratio of the geometric means between the test and the reference, with a 90% confidence interval, of pharmacokinetic parameters for Cmax was 102.26% (94.17-111.04%) and for AUC0-t was 101.24% (95.19-107.68%). Conclusion: Imatinib mesylate 100 mg (test product) from Eurofarma Laboratórios S.A. was considered bioequivalent to the reference Glivec® 100 mg manufactured by Novartis Biociências S.A, and the test product can be interchangeable with the reference, based on their pharmacokinetic performance. https://rbc.inca.gov.br/index.php/revista/article/view/4060imatinib mesylatetherapeutic equivalencytandem mass spectrometrytyrosine protein kinase inhibitors |
| spellingShingle | Carlos Eduardo Sverdloff Vinicius Marcondes Rezende Paulo Alexandre Rebelo Galvinas Guilherme Araújo Pinto Lygia Nerath Bonanato Fernando Bastos Canton Pacheco Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state Revista Brasileira de Cancerologia imatinib mesylate therapeutic equivalency tandem mass spectrometry tyrosine protein kinase inhibitors |
| title | Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state |
| title_full | Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state |
| title_fullStr | Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state |
| title_full_unstemmed | Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state |
| title_short | Bioequivalence/bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus Glivec® in Brazilian healthy male volunteers in fed state |
| title_sort | bioequivalence bioavailability study of a new formulation of imatinib mesylate 100 mg coated tablets versus glivec r in brazilian healthy male volunteers in fed state |
| topic | imatinib mesylate therapeutic equivalency tandem mass spectrometry tyrosine protein kinase inhibitors |
| url | https://rbc.inca.gov.br/index.php/revista/article/view/4060 |
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