Monograph
L01EA01 - Imatinib |
Propably not porphyrinogenic |
PNP |
Rationale
Imatinib is a competative inhibitor of CYP3A4 and 2C9, but there is no data pointing to capacity for mechanism-based inhibition, nor to induction of metabolism of CYP3A4 or 2C9 substrates. Not listed as CYP inducer or irreversible CYP-inhibitor. However, side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Imatinib is an inhibitor of Bcr-Abl tyrosine kinase. The polycyclic molecule contains a secondary amino function.
Therapeutic characteristics
Imatinib is an antineoplastic agents used to treat chronic myelogenous leukemia, malignant gastrointestinal stromal tumors and in dermatofibrosarcoma. It is administered orally. Common adverse reactions of imatinib that can be confused with an acute porphyric attack are nausea, vomiting, diarrhoea, abdominal pain, paraesthesia, myalgia, arthalgia and insomnia. Side effects such as nausea, anorexia and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Imatinib is mainly metabolized by CYP 3A4, while CYPs 1A2, 2D6, 2C9 and 2C19 play lesser roles. Main metabolite is the N-demetylated piperazinederivative. It is a relatively strong competetive inhibitior of of CYPs 3A4/5, 2C9 and 2D6. Imatinib did not exert a significant effect on the PXR-mediated induction of CYP3A4 (Harmsen, 2009). Not listed as CYP inducer or irreversible inhibitor.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Zhou, S.F., Xue, C.C., et al. Clinically important drug interactions potentially involving mechanism-based inhibition of cytochrome P450 3A4 and the role of therapeutic drug monitoring. Ther Drug Monit 2007; 29(6):687:710.
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| 2. | Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor.
Harmsen S, Meijerman I, et al. Cancer Chemother Pharmacol. 2009;64(1):35-43. |
18839173 |
| * | Drug reference publications | |
| 3. | McEvoy GK, editor. Imatinib. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (03.06.10).
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| * | Summary of Product Characteristics | |
| 4. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Glivec.
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Tradenames
This list comprises raw data collected from different countries.
In some cases, a more comprehensive list of available drug packages is included.
Consequently, very similar terms may therefore appear multiple times.
Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
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Bimatix 100 mg filmomhulde tabletten · Bimatix 400 mg filmomhulde tabletten · Glivec 100 mg capsule, harde capsules · Glivec 100 mg filmomhulde tabletten, filmomhulde tabletten · Glivec 400 mg filmomhulde tabletten, filmomhulde tabletten · Imakrebin 100 mg filmomhulde tabletten · Imakrebin 400 mg filmomhulde tabletten · Imatinib Accord 100 mg filmomhulde tabletten · Imatinib Accord 400 mg filmomhulde tabletten · Imatinib Aenorasis, 100 mg filmomhulde tabletten · Imatinib Aenorasis, 400 mg filmomhulde tabletten · Imatinib Amarox 100 mg filmomhulde tabletten · Imatinib Amarox 400 mg filmomhulde tabletten · Imatinib Amarox 600 mg filmomhulde tabletten · Imatinib betapharm 100 mg, filmomhulde tabletten · Imatinib betapharm 400 mg, filmomhulde tabletten · Imatinib CF 100 mg, filmomhulde tabletten · Imatinib CF 400 mg, filmomhulde tabletten · Imatinib Denk 100 mg, filmomhulde tabletten · Imatinib Denk 400 mg, filmomhulde tabletten · Imatinib Devatis 100 mg filmomhulde tabletten · Imatinib Devatis 400 mg filmomhulde tabletten · Imatinib Glenmark 100 mg, filmomhulde tabletten · Imatinib Glenmark 400 mg, filmomhulde tabletten · Imatinib Koanaa 100 mg filmomhulde tabletten · Imatinib Koanaa 400 mg filmomhulde tabletten · Imatinib Krka 100 mg filmomhulde tabletten · Imatinib Krka 400 mg filmomhulde tabletten · Imatinib Sandoz 100 mg, filmomhulde tabletten · Imatinib Sandoz 400 mg, filmomhulde tabletten · Imatinib STADA 100 mg, filmomhulde tabletten · Imatinib STADA 400 mg, filmomhulde tabletten · Imatinib Stada 600 mg filmomhulde tabletten · Imatinib Teva 100 mg, capsules, hard · Imatinib Teva 100 mg, filmomhulde tabletten · Imatinib Teva 400 mg, capsules, hard · Imatinib Teva 400 mg, filmomhulde tabletten · Imatinib Vocate 600 mg, filmomhulde tabletten · Leutipol 100 mg, filmomhulde tabletten · Leutipol 400 mg, filmomhulde tabletten 
Glivec · Glivec 100 mg compr. pellic. · Glivec 100 mg g?l. · Glivec 400 mg compr. pellic. · Imatinib · Imatinib AB 100 mg compr. pellic. · Imatinib AB 400 mg compr. pellic. · Imatinib Accord 100 mg compr. pellic. · Imatinib Accord 400 mg compr. pellic. · Imatinib Actavis 100 mg compr. pellic. · Imatinib Actavis 100 mg g?l. · Imatinib Actavis 400 mg compr. pellic. · Imatinib Actavis 400 mg g?l. · Imatinib Actavis 50 mg g?l. · Imatinib Eurogenerics 100 mg compr. pellic. · Imatinib Eurogenerics 400 mg compr. pellic. · Imatinib Grindeks 100 mg g?l. · Imatinib Krka 100 mg compr. pellic. · Imatinib Krka 400 mg compr. pellic. · Imatinib Teva 100 mg compr. pellic. · Imatinib Teva 100 mg g?l. · Imatinib Teva 400 mg compr. pellic. · Imatinib Teva 400 mg g?l. 
GLIVEC 100 mg CAPSULAS DURAS · GLIVEC 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · GLIVEC 400 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · Imatinib · Imatinib Accord 100 mg comprimidos recubiertos con pelicula · Imatinib Accord 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Accord 400 mg comprimidos recubiertos con pelicula · Imatinib Accord 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Altan 100 mg Capsulas Duras efg · Imatinib Altan 400 mg Capsulas Duras efg · Imatinib Aristo 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Aristo 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Cipla 100 mg Capsulas Duras efg · Imatinib Cipla 400 mg Capsulas Duras efg · Imatinib dr Reddys 100 mg Capsulas Duras efg · Imatinib dr Reddys 400 mg Capsulas Duras efg · Imatinib dr. Reddys 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib dr. Reddys 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Farmalider 100 mg Capsulas Duras efg · Imatinib Farmalider 400 mg Capsulas Duras efg · Imatinib Kern Pharma 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Kern Pharma 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Krka d.d. 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Krka d.d. 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Normon 100 mg Comprimido Recubiertos con Pelicula efg · Imatinib Normon 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Qilu 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Qilu 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Sandoz 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Sandoz 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Swanpond Investments 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Tarbis 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Teva 100 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Teva 400 mg Comprimidos Recubiertos con Pelicula efg · Imatinib Torrefarma 100 mg Capsulas Duras efg · Imatinib Torrefarma 400 mg Capsulas Duras efg 
Glivec · Imanivec · Imatinib 
GLIVEC 100 mg · IMAKREBIN 100 mg · IMAKREBIN 400 mg · IMATINIB ACCORD 100 mg · IMATINIB ACCORD 400 mg · IMATINIB GRINDEKS 100 mg · IMATINIB STADA 100 mg · IMATINIB STADA 400 mg · IMATINIB TERAPIA 100 mg · IMATINIB TERAPIA 400 mg · IMATINIB TEVA 100 mg · IMATINIB TEVA 400 mg · MEAXIN 100 mg · MEAXIN 400 mg 
Glivec · Imatinib · Nibix 
Bimatix · Glivec · Imatinib Accord · Imatinib Amarox · Imatinib Cipla · Imatinib Krka d.d. · Imatinib Sandoz · Imatinib Stada · Imatinib Teva · Imatinib Teva B.V · Imatinib Viatris · Imatinib Zentiva 
Glivec · Imatinib Accord · Imatinib Krka d.d · Imatinib Sandoz · Imatinib Teva 
Glivec · Imatinib Accord · Imatinib Koanaa · Imatinib Sandoz · Imatinib Teva · Imatinib Zentiva · Leuzek · Meaxin · Nibix 
Glivec · Imatinib Accord · Imatinib EG · Imatinib Medac 100mg · Imatinib Medac 400mg · Imatinib Teva 100mg · Imatinib Teva 400mg 
Glivec · Imakrebin · Imatinib Accord · Imatinib Krka d.d. · Imatinib Teva · Imatinib Viatris 
Bimatix · Glivec · Imatinib Accord · Imatinib Krka d.d. · Imatinib Orion · Imatinib ratiopharm · Imatinib Sandoz · Imatinib Stada · Imatinib Teva 
Glivec · Imatinib Accord · Imatinib Grindeks · Imatinib Inteli · Imatinib Teva · Itivas 
Alvotinib® · Glimatin® · Imatinib Grindeks · Meaxin®
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