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Therapeutic combinations of orally administered paclitaxel and a p-gp inhibitor for the treatment of cancer

A paclitaxel and drug delivery technology, which is applied in drug combinations, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve problems such as side effects and tolerance problems

Pending Publication Date: 2018-06-08
ATHENEX THERAPEUTICS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Excipients, such as Cremophor®, used for intravenous administration of paclitaxel, often lead to tolerability problems, e.g., anaphylactic infusion reactions
Intravenous paclitaxel (e.g., Taxol® or paclitaxel formulated in Cremophor®) requires premedication, which has its own side effects

Method used

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  • Therapeutic combinations of orally administered paclitaxel and a p-gp inhibitor for the treatment of cancer
  • Therapeutic combinations of orally administered paclitaxel and a p-gp inhibitor for the treatment of cancer
  • Therapeutic combinations of orally administered paclitaxel and a p-gp inhibitor for the treatment of cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0462] Example 1 - In vivo anti-cancer effect of oral administration of paclitaxel in combination with compound A in tumor cell implanted mouse model active

[0463] The ability of orally administered Paclitaxel in combination with Compound A to inhibit the growth of different human tumor xenograft cell lines was investigated in 7 in vivo experiments in mice. Paclitaxel alone was administered IV or intraperitoneally (IP) as a control. A summary and results of the study are provided in the table below.

[0464] Table 1

[0465]

[0466] In these studies, tumor inhibition rate (IR%) was calculated as ([1 - relative tumor growth in treatment group / relative tumor growth in control group] x 100). Tumor regression was calculated as (mean tumor weight 治疗结束 / average tumor weight 治疗开始 )x100. Thus, a value 100% indicates an increase in tumor weight. Tumor growth delay was calculated as the mean number of days to double tumor mass.

[0467] In all studies, orally administere...

Embodiment 2

[0469] Example 2 - Dose Dependence of Orally Administered Paclitaxel

[0470] In rats and dogs given oral paclitaxel in combination with compound A max and AUC increased more than in a dose-proportional manner, as shown in the table below.

[0471] Table 2: Dose Dependence of Paclitaxel Pharmacokinetics in Rats Following Single Oral Administration in Combination with Compound A

[0472]

[0473] Table 3: Dose Dependence of Paclitaxel Pharmacokinetics in Dogs Following Single Oral Dosing in Combination with Compound A

[0474]

Embodiment 3

[0475] Example 3 - Bioavailability Determination of Orally Administered Paclitaxel in Combination with Compound A in Subjects with Cancer

[0476] A study was designed to determine the absolute bioavailability of orally administered paclitaxel in combination with Compound A in subjects with cancer. Eligible subjects were instructed to take 80mg / m2 once a week over 1 hour 2 Adults treated with intravenous paclitaxel (eg, Taxol® or paclitaxel formulated with Cremophor®).

[0477] The first 6 subjects received the following treatment separately for about 1 week: 80mg / m 2 Paclitaxel (as Taxol® or such) given as IV infusion for 1 hour (on Day 1 or Day 8) plus premedication according to standard local practice; or 15 mg Compound A plus 270 mg (approximately 150 mg / m 2 ) orally administered paclitaxel (days 1 and 2 or days 8 and 9). Compound A was administered 1 hour before oral administration of paclitaxel. No premedication was allowed during this treatment sequence.

[0478]...

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PUM

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Abstract

The application pertains to pharmaceutical combinations of orally administered paclitaxel and a P-gp inhibitor. The pharmaceutical combinations are suitable for the treatment of cancer in a subject and for reducing or preventing toxicity, hypersensitivity -type infusion reactions, and other negative outcomes resulting from or associated with intravenously administered paclitaxel (e.g., Taxol<Registered> or paclitaxel formulated with Cremophor<Registered>) therapy in a subject suffering from cancer.

Description

[0001] related application [0002] This application claims priority and benefit to US Provisional Application 62 / 195,243, filed July 21, 2015, the contents of which are hereby incorporated by reference in their entirety. Background of the invention [0003] Paclitaxel (Taxol ® ) was jointly developed by the National Cancer Institute of the United States and Bristol-Myers Squibb. It was approved by the Food and Drug Administration of the United States as an anticancer drug in 1992 and sold under the trade name Taxol®. Paclitaxel stabilizes microtubules in cells, thereby interfering with the normal fragmentation of microtubules during mitosis. Due to this unique mechanism of inhibiting cancer cell division without deleteriously affecting DNA synthesis, paclitaxel is indicated for the treatment of many types of cancer, including lung, ovarian and breast cancers. [0004] However, paclitaxel's affinity for the p-glycoprotein pump (P-gp) causes paclitaxel to reflux into the inte...

Claims

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Application Information

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IPC IPC(8): A61K31/475A61K31/337A61P35/00
CPCA61K31/337A61K31/4725A61P35/02A61K2300/00
Inventor M.R.关E.D.克拉默G.J.菲特利孔祥德C.G.C.A.杰克逊P.W.格卢
Owner ATHENEX THERAPEUTICS LTD
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