Combination of 17[alpha]-hydroxylase (c17, 20-lyase) inhibitor and specific PI-3K inhibitor for treating tumor disease

A technology of kinase inhibitors and diseases, applied in the field of combined treatment of tumor diseases, can solve problems such as limited treatment options

Inactive Publication Date: 2015-02-11
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Treatment options are significantly limited for cancer patients treated with abiraterone-resistant acetate

Method used

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  • Combination of 17[alpha]-hydroxylase (c17, 20-lyase) inhibitor and specific PI-3K inhibitor for treating tumor disease
  • Combination of 17[alpha]-hydroxylase (c17, 20-lyase) inhibitor and specific PI-3K inhibitor for treating tumor disease
  • Combination of 17[alpha]-hydroxylase (c17, 20-lyase) inhibitor and specific PI-3K inhibitor for treating tumor disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0256] Embodiment 1: clinical trial

[0257] Conduct a clinical study using (a) a phosphatidylinositol 3-kinase inhibitor, which is Compound A or its monotosylate or Compound C or its hydrochloride, in combination with (b) abiraterone acetate or its A pharmaceutically acceptable salt, and (c) prednisone, for the treatment of castration-resistant prostate cancer patients following failure of abiraterone acetate therapy.

[0258]An open-label, open-label study of the combination comprising (a) Compound A or its monotosylate salt or Compound C or its hydrochloride, (b) abiraterone acetate or a pharmaceutically acceptable salt thereof, and (c) prednisone. In Phase 1, a dose escalation study was conducted to determine the maximum tolerated dose (MTD) and / or recommended augmentation dose (RDE) for patients diagnosed with castration-resistant prostate cancer following failure of abiraterone acetate therapy: (a) Combination of compound A or its monotosylate salt with abiraterone ace...

Embodiment 2

[0337] Embodiment 2: clinical research

[0338] Conduct a clinical study using (a) a phosphatidylinositol 3-kinase inhibitor, which is Compound A or its monotosylate or Compound C or its hydrochloride, in combination with (b) abiraterone acetate or its A pharmaceutically acceptable salt, and (c) prednisone, for the treatment of castration-resistant prostate cancer patients following failure of abiraterone acetate therapy.

[0339]An open-label, open-label study of the combination comprising (a) Compound A or its monotosylate salt or Compound C or its hydrochloride, (b) abiraterone acetate or a pharmaceutically acceptable salt thereof, and (c) prednisone. In Phase 1, a dose escalation study was conducted to determine the maximum tolerated dose (MTD) and / or recommended augmentation dose (RDE) for patients diagnosed with castration-resistant prostate cancer following failure of abiraterone acetate therapy: (a) Combination of compound A or its monotosylate salt with abiraterone ...

Embodiment 3

[0459] Example 3: 1-(2-chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (compound D) and compound C or its hydrochloric acid Preclinical studies of salt combinations

[0460] Recently, 1-(2-chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidine-2- In vivo antitumor efficacy of ketones or in combination with compound C or its hydrochloride, a pan-PI3K inhibitor, which model has been established in SCID mice. VCap tumors expressing PTEN and overexpressing wild-type AR were established in chemically castrated mice. LnCap tumors expressing mutant AR(T877A) with PTEN deletion were initially established in non-castrated mice that were chemically castrated at the start of treatment. In 2 separate experiments with the VCap model, 1-(2-chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one treatment (300 mg / kg bid) initially caused slight tumor regression or tumor stasis, followed by tumor growth delay, as shown in Figures 1-2 and Tables 3-6. The ...

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Abstract

The present invention relates to a combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor selected from the group consisting of a compound of formula (I) or a compound of formula (II), or pharmaceutically acceptable salt thereof, (b) a 17alpha-Hydroxylase / C17,20-lyase inhibitor (CYP17 inhibitor), specifically abiraterone acetate and 1-(2-Chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such combination; use of such combination for the treatment of a tumor disease; a commercial package or product comprising such combination; and to a method of treating a patient having a tumor disease comprising administration of said combination to a patient in need thereof.

Description

technical field [0001] The present invention relates to a combination for treating tumor diseases, which comprises simultaneously, separately or sequentially used: (a) a phosphatidylinositol 3-kinase inhibitor selected from a compound of formula (I) or a compound of formula (II) or a pharmaceutically acceptable Salt acceptance, (b) 17α-hydroxylase / C 17,20 - a lyase inhibitor (CYP17) inhibitor or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing the combination; use of the combination in the treatment of tumor diseases; a commercial package or product containing the combination; and treatment A method for a patient with a neoplastic disease, said method comprising administering said combination to a patient in need thereof. Background of the invention [0002] Epidemiological and experimental studies support an important role for phosphatidylinositol 3-kinase (PI3K) in human cancer biology. Activation of PI3K and its downstream effectors ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/00A61K31/4745A61K31/506A61K31/58A61K31/496A61P35/00
CPCA61K31/506A61K31/58A61K31/496A61K31/573A61K31/4745A61K45/06A61K31/444A61K31/5377A61K2300/00A61K31/00A61P13/08A61P35/00A61P35/04A61P43/00
Inventor S·希拉瓦特A·里瓦P·密斯特里
Owner NOVARTIS AG
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