N-Desmethylapalutamide: Difference between revisions
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'''''N''-Desmethylapalutamide''' is a [[nonsteroidal antiandrogen]] (NSAA) and the major [[active metabolite]] of [[apalutamide]], an NSAA which is used as a [[hormonal antineoplastic agent]] in the treatment of [[metastatic]] [[prostate cancer]].<ref name="ErleadaLabel">https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf</ref>{{failed verification}} It has similar activity to that of apalutamide and, with apalutamide therapy, circulates at similar concentrations to those of apalutamide at [[steady state (pharmacokinetics)|steady state]].<ref name="ErleadaLabel" />{{failed verification}} ''N''-Desmethylapalutamide is formed from apalutamide in the [[liver]] by the [[cytochrome P450]] [[enzyme]]s [[CYP2C8]] and [[CYP3A4]].<ref name="ErleadaLabel" />{{failed verification}} |
'''''N''-Desmethylapalutamide''' is a [[nonsteroidal antiandrogen]] (NSAA) and the major [[active metabolite]] of [[apalutamide]], an NSAA which is used as a [[hormonal antineoplastic agent]] in the treatment of [[metastatic]] [[prostate cancer]].<ref name="ErleadaLabel">https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf</ref>{{failed verification|date=May 2021}} It has similar activity to that of apalutamide and, with apalutamide therapy, circulates at similar concentrations to those of apalutamide at [[steady state (pharmacokinetics)|steady state]].<ref name="ErleadaLabel" />{{failed verification|date=May 2021}} ''N''-Desmethylapalutamide is formed from apalutamide in the [[liver]] by the [[cytochrome P450]] [[enzyme]]s [[CYP2C8]] and [[CYP3A4]].<ref name="ErleadaLabel" />{{failed verification|date=May 2021}} |
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==References== |
==References== |
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Revision as of 04:41, 23 May 2021
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| Clinical data | |
|---|---|
| Other names | Desmethylapalutamide; Norapalutamide |
| Drug class | Nonsteroidal antiandrogen |
| Pharmacokinetic data | |
| Protein binding | 95%[1] |
| Identifiers | |
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| PubChem CID | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C20H13F4N5O2S |
| Molar mass | 463.41 g·mol−1 |
| 3D model (JSmol) | |
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N-Desmethylapalutamide is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of apalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer.[1][failed verification] It has similar activity to that of apalutamide and, with apalutamide therapy, circulates at similar concentrations to those of apalutamide at steady state.[1][failed verification] N-Desmethylapalutamide is formed from apalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.[1][failed verification]
References
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