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

A technology of docetaxel, cancer, applied in the field of compound A for treating cancer, compound for treating diseases or disorders

Pending Publication Date: 2021-11-09
ATHENEX HK INNOVATIVE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, intravenously administered docetaxel may also be associated with increased incidence or severity of neurotoxicity

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0855] Example 1 - Clinical study on the combination of multi-west race and compound A for oral administration with IV multi-West

[0856] One study was carried out in a subject with metastatic prostate cancer ("study 1"). The initial stage includes a 21 days of IV application of Dozi Group (according to the dose specified for each participant, as the final treatment of the IV Dauxi His Tour). In the second part of this study, press 75mg / m 2 150mg / m 2 , Or 225mg / m 2 Start, as a single dose, oral dozo. A total of 5 (n = 18) Subjects participated in this study.

[0857] Compared to oral administration, an area is applied from 0 to 24 hours (AUC) 0-24 )higher. The plasma concentration in the multi-West, increases with the increase of IV administration (35, 75mg / m 2 . AUCs for the dose of IV and oral administration were 27.17 (Ng * HR / mL) and 23.33 (Ng * HR / mL), respectively. Half-life for oral dozi, T 1 / 2 It is 21.3h, compared to the half-life of the IV multi-West, is 21....

example 2

[0867] Example 2 - Clinical study on dose surveys of multi-Wests and Compound A combined with oral administration

[0868] One study was carried out in a subject having a solid tumor ("study 2"). Press 35mg / m 2 The initial dose of the starting dose, the maximum tolerated dose (MTD) of Oral Dozi, including 21 days 3 + 3 dose increments. Dosage level is increased to 75 mg / m 2 150mg / m 2 225mg / m 2 300mg / m 2 375mg / m 2 , And 400mg / m 2 . In the second part of this study, a given group starting at half of the dose starting from stage 1 from stage 1 for two days in the second part of this study. A total of 15 (n = 40) subjects participated in this study.

[0869] Pharmacokinetic results from 2 studies showed 35 mg / m 2 75mg / m 2 , And 150mg / m 2 Dose maximum concentration C max The values ​​were 69.1 ng / ml, 172 ng / ml, and 124 ng / ml. Under the 0 to 24-hour curve (AUC 0-24 As the dose increases, 263 ng * hr / ml is for 35 mg / m 2 Oral Dozi, 598 ng * hr / ml for 75mg / ...

example 3

[0876] Example 3 - Comparison of pharmacokinetic characteristics of multi-west race and compound A combined with oral administration (study 1 and research 2)

[0877] The plasma concentration of IV multi-West Herda increases with the increase of dose. Oral dozi he has a similar PK spectrum in two studies. The results are shown in Tables 6 and 7.

[0878] Table 6 Summary of PK parameters in the multi-West

[0879]

[0880] Table 7. Research 1 and Study 2 Title Comparison by Study on Cancer Diagnosis

[0881]

[0882]

[0883] In study, all subjects were diagnosed as prostate cancer. Oral dose is 75mg / m 2 Show C max In the range of 85.6-124 ng / ml, and AUC 0-24 For 313-336 ng * hr / ml. IV dose is 60mg / m 2 Show C max Within 1020-1570 ng / ml, and AUC 0-24 It is 1350-1970 ng * hr / ml.

[0884] In the study 2, cancer diagnosis includes lung cancer, breast cancer, esophageal cancer, lung cancer, urinary tractocarcinoma, pancreatic cancer, cervical cancer, ovarian cancer, an...

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Abstract

The present disclosure provides pharmaceutical combinations of orally administered docetaxel 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 docetaxel (e.g., Taxotere® or docetaxel formulated with polysorbate 80) therapy in a subject suffering from cancer.

Description

[0001] Cross-reference related application [0002] This application claims priority to US Provisional Application No. 62 / 779,742 priority to and the benefit of 14 December 2018 and filed on May 13, 2019, filed 62 / 846,869, and each of said application incorporated herein in its entirety middle. Background technique [0003] Docetaxel In 1995 it was approved for medical use, and to brand name Sales. Docetaxel stable cell microtubules, and thus interfere with the normal division of microtubules during mitosis. Docetaxel for the treatment of various types of cancer (including lung, ovarian and breast cancer). However, docetaxel pump affinity for p- glycoprotein (P-gp) led docetaxel outer race row back to the intestine, so that can not be achieved when the oral bioavailability of the drug. Which is poorly absorbed by the intestinal epithelium, with its adverse solubility, making docetaxel administered intravenously needs. Docetaxel excipients for intravenous administration, such ...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K31/4725A61P35/00A61P35/04
CPCA61K31/337A61K31/4725A61P35/00A61P35/04A61K2300/00A61K9/0019A61K9/0053
Inventor M-F.鲁道夫.关E.D.克雷默D.L.库特勒刘耀南陈荣楷
Owner ATHENEX HK INNOVATIVE LTD
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