AR094654A1 - Modulador del receptor de andrógeno y sus usos, método para tratamiento, composición farmacéutica - Google Patents
Modulador del receptor de andrógeno y sus usos, método para tratamiento, composición farmacéuticaInfo
- Publication number
- AR094654A1 AR094654A1 ARP140100116A ARP140100116A AR094654A1 AR 094654 A1 AR094654 A1 AR 094654A1 AR P140100116 A ARP140100116 A AR P140100116A AR P140100116 A ARP140100116 A AR P140100116A AR 094654 A1 AR094654 A1 AR 094654A1
- Authority
- AR
- Argentina
- Prior art keywords
- prostate cancer
- per day
- dose
- castration
- treatment
- Prior art date
Links
Classifications
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
Abstract
En la presente descripción se describe un modulador de receptores de andrógeno en el tratamiento de cáncer de próstata en combinación con otras opciones terapéuticas y en el tratamiento de enfermedades o condiciones que son tratables con el tratamiento con el modulador de receptor de andrógeno, así como composiciones farmacéuticas y fármacos que incluyen este compuesto. Reivindicación 1: Un método para tratar un paciente humano masculino que padece cáncer de próstata avanzado sensible a la castración, cáncer de próstata resistente a la castración, o cáncer de próstata localizado de alto riesgo; el método comprende administrar el compuesto de la fórmula (1), o una sal farmacéuticamente aceptable de este, en una dosis en un intervalo de aproximadamente 30 mg por día a aproximadamente 480 mg por día a un paciente humano masculino que necesita el tratamiento. Reivindicación 3: Un método para tratar el cáncer de próstata resistente a la castración posterior al tratamiento con acetato de abiraterona, cáncer de próstata metastásico resistente a la castración, cáncer de próstata no metastásico resistente a la castración, cáncer de próstata metastásico sensible a la castración, cáncer de próstata no metastásico sensible a la castración o cáncer de próstata localizado de alto riesgo en un paciente humano masculino; el método comprende administrar por vía oral el compuesto de la fórmula (1), o una sal farmacéuticamente aceptable de este: en la forma de una capsula de gel blando a un paciente que necesita el tratamiento, en una dosis de aproximadamente 30 mg por día a aproximadamente 480 mg por día, preferentemente, en una dosis de aproximadamente 240 mg por día en combinación con: (a) un inhibidor de fosfoinositida 3-quinasa (Pl3K), inhibidor de TORC, o inhibidor doble de PI3K/TORC, preferentemente, everolimus, BEZ-235, BKM120, BGT226, BYL-719, GDC0068, GDC-0980, GDC0941, GDC0032, MK-2206, OSI-027, CC-223, AZD8055, SAR245408, SAR245409, PF04691502, WYE125132, GSK2126458, GSK-2636771, BAY806946, PF-05212384, SF1126, PX866, AMG319, ZSTK474, Cal101, PWT33597, LY-317615 (clorhidrato de enzastaurina), CU-906, o CUDC-907, y si el inhibidor de TORC es everolimus, se administra en una dosis de aproximadamente 5 mg por día a aproximadamente 20 mg por día; o (b) un inhibidor de quinasa, preferentemente, en donde el inhibidor de quinasa es: (i) un inhibidor de quinasa MET o VEGFR, con mayor preferencia, Cabozantinib (XL184), PF-2341066 (Crizotinib), ARQ-197 (Tivantinib), MK-2461, JNJ-38877605, MK-8033, INCB-28060, BMS-777607, AMG-208, LY-2801653, EMD-1214063, EMD-1204831, AMG-337, HMPL-504 (Volitinib), SAR-125844, LY2875358, ABR-215050 (Tasquinimod), CHIR-258 (Dovitinib), EXEL-7647, OSI-930, BIBF-1120, BAY-73-4506 (Regorafenib), BMS-582664 (Brivanib), JNJ-26483327, AZD-2171 (Cediranib), Sorafenib, Aflibercept, Enzastaurin, AG-013736 (Axitinib), OSl-632, o GSK-786034 (Pazopanib), y si es Cabozantinib, se administra por vía oral en una dosis de aproximadamente 40 mg por día a aproximadamente 100 mg por día; o (ii) un inhibidor de quinasa EGFR, MEK, o SRC, con mayor preferencia, Erlotinib, Cetuximab, Gefitinib, Canertinib, Panitumumab, Nimotuzumab, Lapatinib, Vandetanib, Afatinib, MP-412, AEE-788, Neratinib, XL-647, AC-480, Dacomitinib, AZD-8931, CUDC-101, AP-26113, CO-1686, Trametinib, Selumetinib, MEK-162, Refametinib, TAK-733, R0-5126766, Bl-847325, AZD6244, GSK1120212, PF-5208763 (Bosutinib), o AZD-0530 (Saracatinib), y si es Erlotinib, se administra por vía oral en una dosis en un intervalo de aproximadamente 100 mg a aproximadamente 150 mg; y si es Gefitinib, se administra por vía oral en una dosis de aproximadamente 250 mg; y si es Trametinib, se administra por vía oral en una dosis de aproximadamente 1 mg a aproximadamente 2 mg; o (iii) un inhibidor de quinasa AKT, RAF, FGFR, o CDK4/6, con mayor preferencia, GDC0068, MK-2206, AT7867, GSK2110183, GSK2141795, GSK690693, Vemurafenib (PLX4032/RG7204), GSK2118436, Dabrafenib (GSK208436), LGX818, RAF265, LY2780301, Dovitinib (TKl258), BGJ398, AZD4547, PD-0332991 o LEE011.
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ARP190103469A AR117670A2 (es) | 2013-01-15 | 2019-11-27 | Modulador del receptor de andrógeno y sus usos |
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