Sensitizer drug, pharmaceutical composition and application

A technology of sensitizers and drugs, applied in the field of biomedicine, can solve the problems of lack of specificity, effective cell permeability, etc., and achieve the effect of improving sensitivity, enhancing sensitivity, and wide targeting.

Active Publication Date: 2020-09-18
SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, previously discovered Pin1 inhibitors lack specificity, potency and / or cell permeability

Method used

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  • Sensitizer drug, pharmaceutical composition and application
  • Sensitizer drug, pharmaceutical composition and application
  • Sensitizer drug, pharmaceutical composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] In vitro and in vivo biological tests

[0054] (1) Materials and methods

[0055] (1) Drugs

[0056]ATRA (Sigma) was dissolved in 150 mM DMSO and diluted in 1:1 PBS and 1M NaOH working solution and administered intraperitoneally in 200 ml at a dose of 1.5 mg / kg once a day. Olaparib (Selleckchem) was formulated and used as described in the literature Cancer Discov. 2012; 2: 1048-63.

[0057] (2) Cells and cell culture

[0058] MCF10A cells derived from ATCC were cultured in DMEM / F-12, adding 5% horse serum, 20ng / ml epidermal growth factor (EGF), 0.5μg / ml hydrocortisone, 100ng / ml cholera toxin, 10μg / ml insulin, Culture was as described in the literature Methods.2003; 30: 256-68. ATCC-derived MCF-7, T47D, MDA-MB 231, AU565, HEK293 were cultured in DMEM containing 10% FBS. SUM149 was cultured in Ham's F-12 medium containing 5% bovine serum (FBS), insulin (5 μg / mL) and hydrocortisone (2 μg / mL).

[0059] Choose the radiation dose according to the experiment and the cell...

Embodiment 2

[0088] Pharmaceutical composition containing all-trans retinoic acid 10 mg and olaparib 100 mg

[0089] 10 grams of all-trans retinoic acid and 100 grams of olaparib were crushed through a 120 mesh sieve respectively, and then mixed with 25 grams of croscarmellose sodium, 20 grams of mannitol, and 15 grams of polysaccharides crossed through an 80 mesh sieve. Vitone was mixed evenly, and 30 grams of 10% starch slurry was added to make soft materials, granulated through a 24-mesh sieve, then ventilated and dried at 50 degrees Celsius, and after granulation with a 20-mesh sieve, mixed with 2 grams of colloidal silicon dioxide and 2 2.5 grams of sodium stearyl fumarate is mixed uniformly, and compressed into tablets to obtain pharmaceutical composition tablets.

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PUM

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Abstract

The invention discloses a sensitizer drug, a pharmaceutical composition and application. A sensitizer in the invention is a Pin1 inhibitor; the clinical effect of tumour targeting therapy is easily improved by inhibiting prolyl isomerase Pin1 and improving the sensibility of expression of BRCA1 breast cancer on a PARP inhibitor; in addition, the pharmaceutical composition of the Pin1 inhibitor andthe PARP inhibitor in the invention can be used for preparing a therapeutic drug targeting HR sensitive tumours, and can be used for treating BRCA1 wild type cancers; and furthermore, the pharmaceutical composition is good in security and low in toxicity.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a sensitizer drug, drug combination and application thereof, in particular to a sensitizer drug, drug combination and application for enhancing the sensitivity of PARP inhibitor radiotherapy and chemotherapy for cancers expressing BRCA1 . Background technique [0002] BRCA1 protein is phosphorylated in response to DNA damage, and phosphorylation is necessary for the DNA damage repair function of BRCA1 (Science, 1999; 286: 1162-6, Nature, 2000; 404: 201-4). Loss of BRCA1 function predisposes to breast or ovarian cancer. Furthermore, BRCA1 loss of function predicts differential responses to defective DNA damage repair: breast, ovarian, prostate, and pancreatic cancer patients with BRCA1 mutations are sensitive to therapeutic PARP inhibition, whereas PARP inhibition due to homologous recombination (HR) deficiency Can cause insurmountable DNA damage. PARP inhibitors have emerged...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K45/06A61K31/203A61K33/36A61K31/122A61K31/502A61P35/00
CPCA61K45/00A61K45/06A61K31/203A61K33/36A61K31/122A61K31/502A61P35/00A61K2300/00
Inventor 胡海罗曼莉郑芳
Owner SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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