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Triterpenoid antifungals for the treatment of fungal osteo-articular infections

A fungal, osteoarticular technology, used in the treatment of osteofungal infections and related connective tissue fungal infections, fungal infections, and can solve problems such as limited bone penetration

Pending Publication Date: 2021-10-12
SCYNEXIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for most conventional antifungal agents, drug penetration into bone is limited

Method used

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  • Triterpenoid antifungals for the treatment of fungal osteo-articular infections
  • Triterpenoid antifungals for the treatment of fungal osteo-articular infections
  • Triterpenoid antifungals for the treatment of fungal osteo-articular infections

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0116] Evaluation of Clinical Efficacy of SCY-078 Treatment of Osteogenic Fungi infection

[0117] This example shows the treatment process of patients with two candideline discitis, they participated in the "Assessment of the Efficacy and Safety of SCY-078 in the refractory or non-tolerated fungal disease (FURI) patients NCT03059992) (CLINICALTRIALS.GOV identifier NCT03059992).

[0118] OBJECTIVE: The study of the study is to assess the efficacy of oral administration of SCY-078 treatment to approved antifungal agents or non-tolerant fungal infections.

[0119] Research Design: This is a multi-center, open label, non-comparison, single arm research, aimed at assessing SCY-078 (as citrate application) in affocacy and / or severe candida disease in patients with records ≥ 18 years old Male and female subjects in the effects, safety and pharmacokinetics (PK) of the ethnoplastin disease, which is refractory or non-tolerant or description of standard care (SOC) antifungal treatment or...

example A

[0122] Example A: A 50-year-old male, diagnosed as acute myeloid leukemia (AML), before receiving the same kind of foreign stem cell transplantation (SCT) and graft anti-main disease (GVHD), suffering from L4 / L5 white candida inflammation. Five months ago, the patient had two white candida primer alpacaramia, and fungal blood contained four days and 7 days respectively. The patient participated in FURI studies and was treated with an oral Ai Ruifen (750 mg BID for 2 days, then 750 mg QD daily). After L4 / L5, the backpack vertebrae fusion (PLIF). At the time of assessment, the patient has been used in oral Ai Ruofen. 277 days. Due to pain relief, refundlacing and activity improvement, the assessment of patient responses has been rated as improved. Possible research drug-related adverse events is diarrhea, gastrointestinal air deflation and nausea.

example B

[0123] Example B: A 58-year-old male, bladder cancer is recurrent after retreating of radical bladder regeneration in the ileal catheter, suffering from L5 / S1 tropical candida. Three months ago, he had a tropical candida antifungalmia. The patient participated in FURI studies and was treated with an oral Ai Ruifen (750 mg BID for 2 days, then 750 mg QD daily). At the time of assessment, the patient has been used in oral Ai Ruofen to treat 88 days. Due to the retardation of clinical symptoms, the assessment of patient responses has been rated to date. Possible research drug-related adverse events is diarrhea.

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PUM

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Abstract

Enfumafungin derivative triterpenoid antifungal compounds are used to treat osteo-articular fungal infections, due to their unexpected bone tissue penetration and associated efficacy for such infections. The enfumafungin derivative triterpenoids (or pharmaceutically acceptable salts or hydrates thereof) are inhibitors of (1,3)-[beta]-D-glucan synthesis and are useful in the treatment of yeast or mold infections that occur in osteo-articular structures such as osteomyelitis, spondylodiscitis, and arthritis.

Description

Technical field [0001] The present invention relates to Enfumafen net (enfumafungin) triterpene derivative antifungal compounds for the treatment of fungal infections of bone (including osteomyelitis) and related connective tissue (e.g., bone and joint periosteum and other tissues, including but not limited to bone marrow , use of joint fluid, cartilage, intervertebral discs, and other structures, etc.) fungal infections (collectively referred to as "bone and joint infections" in this disclosure) is. More particularly, the present invention relates to a (1,3) -β-D- Enfumafen glucan synthesis inhibitors net triterpene derivative (or a pharmaceutically acceptable salt or hydrate thereof) in the treatment of bone It occurred in the joint structure and long-term antifungal therapy (over 4 weeks) and sufficient affected tissue penetration of the antifungal fungal infections regression of infection (e.g., yeast or fungal infection) uses. (1,3) -β-D- glucan synthesis inhibitors are consi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P31/10
CPCA61K31/56A61P31/10A61K31/4409
Inventor D·A·安古洛·冈萨雷斯
Owner SCYNEXIS INC
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