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Use of itraconazole in preparation of drug for treating multiple myeloma

A technology for multiple myeloma and itraconazole, which is applied in the field of tumor treatment and can solve problems such as refractory anemia and anti-infection treatment

Inactive Publication Date: 2012-08-01
万礼 +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] 3. Anemia and infection may be difficult to give symptomatic anti-anemia and anti-infection treatment

Method used

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  • Use of itraconazole in preparation of drug for treating multiple myeloma
  • Use of itraconazole in preparation of drug for treating multiple myeloma
  • Use of itraconazole in preparation of drug for treating multiple myeloma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1, animal test

[0027] Medication method; Oral

[0028] Experimental conditions: Clean grade C57BL / KaLwRijHsd mice were used, purchased from Harlan Company in the Netherlands. C57BL / KaLwRijHsd mice were raised and tested in a clean laboratory.

[0029] Test drug: inject itraconazole (produced by SIGMA Company of the United States), and dissolve itraconazole in dimethyl sulfoxide (produced by SIGMA Company of the United States) to prepare a solution.

[0030] Test method: Take 20 6-week-old C57BL / KaLwRijHsd mice and divide them into 2 groups, with half male and half male animals in each group, and there is no statistically significant difference in body weight among the animals in each group.

[0031] The dosing regimen for the two groups of animals is:

[0032] Control group: dimethyl sulfoxide, 0.1ml / kg body weight / day

[0033] Treatment group: itraconazole 20mg / kg body weight / day (drug concentration 4mg / ml)

[0034] One week after C57BL / KaLwRijHsd mic...

Embodiment 2

[0036] Embodiment 2 liver and kidney toxicity test

[0037] Test drug: itraconazole;

[0038] Comparing drug: bortezomib.

[0039] Test animals: mice.

[0040] Test method: refer to the "Guiding Principles of Drug Toxicology Research"

[0041] Test results: Compared with bortezomib, itraconazole has less liver and kidney toxicity, and no accidental death due to drug toxicity occurred in the mouse test.

Embodiment 3

[0042] Embodiment 3 human body test

[0043] Referring to the "Technical Guidelines for Clinical Trials of Antineoplastic Drugs", select 30 patients, 20 males and 10 females, aged 30-65 years, and the observation indicators include overall survival, disease-free survival, progression-free survival, and disease progression. time to treatment failure, subject-reported outcomes and quality of life, improvement in signs and symptoms (weight gain, pain reduction).

[0044] The main symptoms were renal insufficiency in 19 cases, anemia in 17 cases, bone damage in 16 cases, fatigue in 6 cases, hypercalcemia in 2 cases, and extramedullary plasmacytoma in 1 case. Some patients have more than two symptoms. Clinical stage: 3 cases in stage I, 8 cases in stage II, and 19 cases in stage III. Bone damage was confirmed by x-ray, CT or MRI, and whole-body bone scan. The test results showed that among the 30 patients, there were 11 cases of IgG type, 10 cases of light chain type, 6 cases of...

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Abstract

The invention discloses a drug for treating multiple myeloma and especially relates to a use of itraconazole or its salts in preparation of a drug composition for treating multiple myeloma. It is accidentally discovered that itraconazole has effects of treating multiple myeloma. A treatment principle of itraconazole comprises that itraconazole mainly acts on a cancer cell Hedgehog (Hh) signal path and inhibits accumulation of Smoothened (Smo) protein in the cancer cell Hedgehog (Hh) signal path thereby inhibiting growth of cancer cells. Compared with bortezomib, itraconazole has small liver and kidney toxicity. Accidental death is not produced due to drug toxicity in a mouse test. A result of a clinical experiment shows that itraconazole has effects of treating various types of multiple myeloma and especially has good treatment effects after bone marrow transplantation. Results of treatment on 30 clinical tested patients show that a total effective rate is 95.9%. In addition, through combination with bortezomib, itraconazole has better effects.

Description

technical field [0001] The invention belongs to the field of tumor treatment and relates to a medicine for treating multiple myeloma. Background technique [0002] Itraconazole is a synthetic azole broad-spectrum antifungal drug, used for systemic infections caused by deep fungi, and can also be used for candidiasis and aspergillosis. [0003] Molecular formula: C35H38C12N8O4 [0004] Molecular weight: 705.64 [0005] CAS number: 84625-61-6 [0006] Chemical name: cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazolyl-1-methanol base) [0007] The structural formula is: [0008] [0009] Itraconazole belongs to triazole broad-spectrum antifungal drugs, and exerts its antifungal effect by inhibiting the biosynthesis of ergosterol, an essential component of fungal cell membranes. Itraconazole has a complete dosage form, including intravenous preparations, oral capsules and oral solutions. Its new dosage form is oral solution and intravenous preparation, which ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P35/00
Inventor 万礼杨烨王旻
Owner 万礼
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