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Application of famitinib in preparation of medicine for treating tumor with c-KIT or PDGFRA mutation

A use and technology of tinib, which can be applied in the direction of antineoplastic drugs, drug combinations, pharmaceutical formulations, etc., and can solve problems such as treatment failure

Pending Publication Date: 2021-12-31
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although imatinib is effective in the treatment of GIST, more than 50% of patients have treatment failure after 2 years of imatinib treatment, and about 14% of patients have disease progression after 6 months of treatment

Method used

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  • Application of famitinib in preparation of medicine for treating tumor with c-KIT or PDGFRA mutation
  • Application of famitinib in preparation of medicine for treating tumor with c-KIT or PDGFRA mutation
  • Application of famitinib in preparation of medicine for treating tumor with c-KIT or PDGFRA mutation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Cell Proliferation Inhibition Experiment

[0041] 1. Famitinib, sunitinib and imatinib inhibit the proliferation of 32D cells transfected with various c-KIT mutations

[0042] Materials and methods

[0043] Compounds: famitinib malate, imatinib mesylate and sunitinib malate were synthesized and provided by Jiangsu Hengrui Pharmaceutical Co., Ltd. (Jiangsu Province, China).

[0044] site-directed mutagenesis

[0045] Michael H. Tomasson (Washington University School of Medicine, St. Louis, MO, USA) generously provided a murine stem cell virus-based retroviral construct carrying a mouse-human heterozygous WT KIT cDNA or the activating mutant D816V (816Asp→ Val) KIT cDNA. A heterozygous KIT allele is generated by in-frame fusion of the extracellular and transmembrane domains of murine KIT with the intracellular domain of human KIT. Studies have shown that replacement of the human extracellular and transmembrane domains of KIT with homologous murine sequen...

Embodiment 2

[0065] Example 2: Multicenter, open, single-arm phase II clinical trial dosing regimen of famitinib malate in the treatment of gastrointestinal stromal tumors

[0066] Famitinib 25 mg orally before breakfast daily. The dose can be lowered to 20mg / d according to the side effects; continuous administration for 28 days is a treatment cycle, and the drug should be taken at roughly the same time every day as much as possible. During the period, if toxic side effects occur, the administration can be suspended, and the suspension of administration time will be included in the treatment cycle. The initial dose of famitinib is 25 mg, and if the dose needs to be lowered due to toxicity, it is allowed to be lowered to 20 mg / d.

[0067] Inclusion criteria

[0068] Patients must meet all of the following inclusion criteria to be enrolled in the trial:

[0069] 1) Male or female, aged 18-75 years;

[0070] 2) Patients with metastatic recurrence / unresectable GIST diagnosed by histopathol...

Embodiment 3

[0114] Example 3: A randomized, open-label, controlled, multi-center phase III clinical study of famitinib malate versus sunitinib malate in the treatment of gastrointestinal stromal tumors that failed imatinib treatment

[0115] Dosing regimen

[0116] test group:

[0117] Famitinib: Oral administration, 25mg / time, once a day, before or after meals. It is recommended to take the drug at a fixed time every day, within 0.5 hours after a meal, and every 6 weeks is a treatment cycle. Dose adjustments and dosing delays are allowed.

[0118] Control group:

[0119] Sunitinib: Oral administration, 50mg / time, once a day, can be administered before or after meals, it is recommended to administer at a fixed time every day, taking 4 weeks and stopping for 2 weeks, every 6 weeks is a treatment cycle. Dosage adjustment and delayed administration are allowed, please refer to the drug instructions for specific administration and adjustment schemes.

[0120] Inclusion criteria

[0121...

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Abstract

The invention relates to an application of famitinib or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating tumors with c-KIT or PDGFRA mutation. Specifically, the invention relates to application of famitinib or a pharmaceutically acceptable salt thereof in preparation of medicines for treating gastrointestinal stromal tumor, testicular spermatogonoma, mastocyte diseases, melanoma or acute myeloid leukemia with c-KIT or PDGFRA mutation.

Description

technical field [0001] The disclosure belongs to the field of medicine, and relates to the use of famitinib or a pharmaceutically acceptable salt thereof in the preparation of medicines for treating c-KIT or PDGFRA mutated tumors. Background technique [0002] Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tissue-derived tumor of the gastrointestinal tract, with an incidence of about 1 / 100,000 to 2 / 100,000 people, accounting for 1 / 100,000 to 2 / 100,000 people. 1% to 4% of tumors. Most commonly occurs in the stomach (60% to 70%), followed by the small intestine (20% to 30%), the colorectum accounts for only 5%, and the esophagus is less than 5%, and occasionally occurs in the retroperitoneum, mesentery, omentum, etc. The median age of GIST is 50 to 60 years old, and it is rare before the age of 40. The younger the age of onset, the greater the possibility of malignancy; there is no significant difference between genders, but small intestinal stromal tumo...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61P35/00A61P1/00
CPCA61K31/437A61P35/00A61P1/00
Inventor 王泉人任文明杨清杨昌永
Owner JIANGSU HENGRUI MEDICINE CO LTD
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