喷他脒依西酸盐(Pentamidine Isethionate) - 在研适应症：肺孢子菌肺炎，心肌梗塞_专利_临床

概要

基本信息

药物类型

小分子化药

别名

1,5-bis(4-amidinophenoxy)pentane、4,4'-(1,5-pentanediylbis(oxy))bis-benzenecarboximidamide、4,4'-(pentamethylenedioxy)dibenzamidine

+ [19]

靶点-

作用方式-

作用机制-

治疗领域

感染呼吸系统疾病其他疾病+ [1]

在研适应症

肺孢子菌肺炎心肌梗塞

非在研适应症

晚期胰腺腺癌肝细胞癌结肠转移性腺癌+ [2]

原研机构

Fresenius Kabi AG

在研机构

Fresenius Kabi USA LLC

Medical College of WisconsinSanofi KK

非在研机构

Verlyx Pharma, Inc.

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (1984-10-16),

肺孢子菌肺炎

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C23H36N4O10S2

InChIKeyYBVNFKZSMZGRAD-UHFFFAOYSA-N

CAS号140-64-7

关联

40

项与喷他脒依西酸盐相关的临床试验

NCT03730363

/ Completed临床1期IIT

A Phase I Study of Pentamidine in Combination With Salvage Chemotherapy for Relapsed/Refractory Classical Hodgkin Lymphoma

Primary Objective:
To evaluate dose limiting toxicity and to determine the recommended phase 2 dose (RP2D) of pentamidine in combination with salvage chemotherapy with ifosfamide, carboplatin and etoposide (ICE) on a 3-weeks schedule in relapsed/refractory classical Hodgkin lymphoma (cHL).
Secondary Objective:
* To estimate the overall best treatment response at 5- and 16-weeks from study enrollment. Although the clinical benefit of these drugs in combination has not been established, offering this treatment may provide a therapeutic benefit. The patients will be carefully monitored for tumor response and symptom relief, in addition to safety and tolerability.
* To estimate the duration of response to the proposed combined therapy.
* To measure the protein of regenerating liver-3 (PRL-3) level of expression in patients at time of relapse.
* To measure circulating biomarkers of response (soluble CD30 (sCD30), and thymus and activation-related chemokine (TARC)) in serum samples collected throughout treatment and inhibition of (pSTAT, pAKT) in peripheral blood mononucleated cells (PBMC).
Exploratory Objective:
* To measure cell-free messenger RNA (cfmRNA) in peripheral blood.
* To measure cell-free DNA in peripheral blood

开始日期2018-12-19

申办/合作机构

University of Kentucky

NCT03403621

/ Terminated临床1/2期IIT

Double Blind, Single-Center, Randomized, Within Subject Placebo, Phase I Study Evaluating the Effects of Novel Topical Gel in Prevention of Hypertrophic Scar Formation

Researchers are trying to find out more about the side effects of topical (applied to the skin) Pentamidine, to determine if it is safe for use in people. They also want to find out if topical use of Pentamidine can help treat hypertrophic scars.
Pentamidine is a medicine that is currently used to treat certain kinds of infection. It is most often given by intravenous (into a vein) or inhalation (through a breathing device). This medication is approved by the U.S. Food and Drug Administration (FDA) for use in these forms.
Everyone in this study will receive topical Pentamidine (TP) in a silicone based gel (PCCA Pracasil Plus). Topical treatment of Pentamidine is still experimental and has not been formally tested for safety or effectiveness in a randomized control trial within the United States. The FDA has allowed the use of topical Pentamidine in this research study.

开始日期2018-03-05

申办/合作机构

Mayo Clinic

NCT03201159

/ Withdrawn临床1期IIT

A Pilot, Exploratory Dose Escalating Study on the Safety, Pharmacodynamics and Preliminary Efficacy of VLX103 in the Treatment of Moderate Alcoholic Steatohepatitis

The study drug (VLX103) is being developed for the treatment of Alcoholic Steatohepatitis and other liver diseases. Alcoholic Steatohepatitis is an inflammatory (associated with irritation, swelling and cell damage) disease that affects the liver. It is associated with heavy and chronic intake of alcohol and presence of fat in the liver. Signs and symptoms often include fever, yellowing of the skin, nausea and impairment of liver function.
The main objective of this study is to evaluate the safety, pharmacodynamics (what the drug does to the body) and pharmacokinetics (how the drug is handled by the human body, like absorption and elimination) of increasing doses of VLX103 in subjects with moderate Alcoholic Steatohepatitis. In other words, we will evaluate how your body tolerates VLX103 at a specific dose and the effects that this VLX103 dose has on your liver and your body in general. The secondary objectives of this study are to evaluate if VLX103 has the potential to treat Alcoholic Steatohepatitis patients, to determine the maximum dose that can be tolerated, and to measure the levels of VLX103 in your blood at different time points during the study.
VLX103 is an experimental drug. Experimental means that the drug has not been approved by the Food and Drug Administration (FDA) for the treatment of Alcoholic Steatohepatitis. The active ingredient in VLX103, pentamidine, is approved for treating parasitic (microorganisms) infections. Pentamidine is currently approved and marketed in about 20 countries, including the United States, for use by injection (administered by a syringe) and by inhalation (administered by a nebulizer) for other health conditions. However, VLX103 is the first oral form of pentamidine being developed, and is administered by mouth as an oral tablet.

开始日期2017-06-25

申办/合作机构

National Institute on Alcohol Abuse & Alcoholism

[+3]

100 项与喷他脒依西酸盐相关的临床结果

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100 项与喷他脒依西酸盐相关的转化医学

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100 项与喷他脒依西酸盐相关的专利（医药）

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3,332

项与喷他脒依西酸盐相关的文献（医药）

2025-08-05·Microbiology Spectrum

Pentamidine inhibition of streptopain attenuates Streptococcus pyogenes virulence

Article

作者: Trivedi, Keya ; LaRock, Christopher N.

ABSTRACT:

The obligate human pathogen Streptococcus pyogenes (also known as GAS; Group A Streptococcus ) carries high morbidity and mortality, primarily in impoverished or resource-poor regions. The failure rate of monotherapy with conventional antibiotics is high, and invasive infections by this bacterium frequently require extensive supportive care and surgical intervention. Thus, it is important to find new compounds with adjunctive therapeutic benefits. The conserved secreted protease streptopain (Streptococcal pyogenic exotoxin B; SpeB) directly contributes to disease pathogenesis by inducing pathological inflammation, degrading tissue, and promoting the evasion of antimicrobial host defense proteins. This study screened 400 diverse off-patent drugs and drug-like compounds for inhibitors of streptopain proteolysis. Lead compounds were tested for activity at lower concentrations and anti-virulence activities during in vitro infection. Significant inhibition of streptopain was seen for pentamidine, an anti-protozoal drug approved for the treatment of Pneumocystis pneumonia, leishmaniasis, and trypanosomiasis. Streptopain inhibition rendered GAS susceptible to killing by human innate immune cells. These studies identify unexploited molecules as new starting points for drug discovery and a potential for repurposing existing drugs for the treatment of infections by GAS.

IMPORTANCE:

Streptococcus pyogenes is a common cause of severe invasive infections. Repeated infections can trigger autoimmune diseases such as acute rheumatic fever and rheumatic heart disease. This study examines how targeting a specific, highly conserved virulence factor of the secreted cysteine protease streptopain can sensitize a serious pathogen to killing by the immune system. Manipulating the host-pathogen interaction, rather than attempting to directly kill a microbe, is a promising therapeutic strategy. Notably, its benefits include limiting off-target effects on the microbiota. Streptopain inhibitors, including the antifungal and antiparasitic drug pentamidine as identified in this work, may therefore be useful in the treatment of S. pyogenes infection.

2025-08-01·INTERNAL MEDICINE

Comparison between the Outcomes of Pentamidine and Trimethoprim-Sulfamethoxazole for <i>Pneumocystis</i> Pneumonia in Non-HIV Patients: A Nationwide Japanese Retrospective Cohort Study

Article

作者: Fushimi, Kiyohide ; Yasunaga, Hideo ; Aso, Shotaro ; Matsui, Hiroki ; Taniguchi, Jumpei

Objective Data on the first-line treatment options for patients with Pneumocystis pneumonia (PCP) without human immunodeficiency virus (HIV) infection are limited. Therefore, we evaluated the outcome of pentamidine compared to trimethoprim-sulfamethoxazole (TMP-SMX) in non-HIV patients with PCP. Methods We used data from the Japanese Diagnosis Procedure Combination Inpatient Database. We included non-HIV PCP patients who initially received TMP-SMX or pentamidine between July 2010 and March 2022. We categorized eligible patients into TMP-SMX and pentamidine groups and performed a propensity score overlap weighting analysis to compare in-hospital mortality between the groups. Results Among 5,870 eligible patients, 5,456 and 414 received TMP-SMX and pentamidine, respectively. Pentamidine treatment was associated with a higher in-hospital mortality than TMP-SMX treatment in the propensity score overlap weighting analysis (23.6% vs. 40.1%; risk difference, 16.5%; 95% confidence interval, 10.8-22.2%; p<0.001). Conclusions Based on these findings, pentamidine may not be as effective as TMP-SMX for treating PCP in non-HIV patients.

2025-07-19·Scientific Reports

Efficient adsorption of basic fuchsin dye using thermally engineered novel smart nanocomposites.

Article

作者: Abdelrahman, Ehab A

Basic fuchsin dye is known for its genotoxic, neurotoxic, and carcinogenic effects on humans and its long-term persistence and ecological toxicity in aquatic environments. In this study, novel MgO/BaCO₃/BaCrO₄/C nanocomposites were fabricated through a Pechini-type sol-gel strategy and thermally treated at 600 and 800 ^oC to yield MB600 and MB800, respectively, for the effective adsorption of basic fuchsin from water-based solutions. The crystalline phases were identified using X-ray diffraction patterns, indicating the formation of crystalline MgO, BaCO₃, and BaCrO₄ phases, with average crystallite sizes of 60.70 and 75.64 nm for MB600 and MB800, respectively. Energy dispersive X-ray spectroscopy revealed the atomic composition, with MB600 containing 21.3% C, 51.1% O, 10.2% Mg, 2.8% Cr, and 14.6% Ba, while MB800 showed enhanced metal content and reduced carbon residues. Field emission scanning electron microscope and high-resolution transmission electron microscope micrographs demonstrated morphological evolution with increasing calcination temperature and average particle sizes of 13.7 and 32.1 nm for MB600 and MB800, respectively. MB600 exhibited a maximum adsorption capacity of 442.48 mg/g, outperforming MB800 at 375.94 mg/g. The sorption mechanism was spontaneous, exothermic, physisorption, and best described by the pseudo-first-order model in addition to the Langmuir isotherm, demonstrating monolayer coverage and uniform surface binding.

1

项与喷他脒依西酸盐相关的新闻（医药）

2024-03-07

·Business Wire

Montdorex Announces Acceptance of Its Abstract for Presentation at the AACR Annual Meeting 2024

MONTREAL--( BUSINESS WIRE )--Montdorex Inc. (“Montdorex” or “the Company”), a privately-owned precision medicine company, today announced that Terry Chow, Ph.D., Founder and CEO will present insights on the relevance of inhibiting the endo-exonuclease (EE) enzyme in a poster presentation at the American Association for Cancer Research (AACR) Annual Meeting, to be held in San Diego, CA, April 5-10, 2024. The endo-exonuclease enzyme plays a key role in DNA damage repair mechanisms, but it is also overexpressed in cancer tumors. In a proof-of-concept study, Montdorex showed that tumors with increased EE expression showed the best response to pentamidine, an endo-exonuclease inhibitor. The Company has also identified mono- and di-amidine analogs of pentamidine that are more effective than the parent drug in both in vitro and in vivo studies. “Our lead candidate, MTDX203, showed an increased anti-cancer activity with a higher safety index than pentamidine in preclinical animal studies,” said Terry Chow of Montdorex. “I look forward to presenting our detailed findings to the AACR scientific and investor community at the upcoming annual meeting.” Details of the AACR poster presentation are as follows: Poster Presentation (#5604): Modulating DNA repair through endo-exonuclease inhibition: a new therapeutic paradigm in Oncology [ link to the abstract ] Session Category: Molecular/Cellular Biology and Genetics Session Title: DNA Damage and Repair 2 Session Date and Time: Tuesday, April 9, 2024 1:30 PM – 5:00 PM (PT) Location: Poster Section 14, Poster Board Number 2 About Montdorex Based in Montreal, Canada, Montdorex Inc. is a privately-owned, early-stage precision medicine company, targeting the endo-exonuclease (EE) enzyme involved in cancer tumor growth and inflammatory processes. The company is developing proprietary mono-amidine and di-amidine EE inhibitors to modulate DNA repair in oncology and non cytotoxic di-amidine analogs for anti-inflammatory applications, such as gastrointestinal conditions and liver diseases. For more information, please visit montdorex.com .

AACR会议临床结果

100 项与喷他脒依西酸盐相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00834	喷他脒依西酸盐	P01CX01	DB00738

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
肺孢子菌肺炎	美国	Fresenius Kabi USA LLC	1984-10-16

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
转移性非小细胞肺癌	临床2期	波兰	Verlyx Pharma, Inc.	2012-09-01
转移性结直肠癌	临床2期	加拿大	Verlyx Pharma, Inc.	2011-03-01
晚期胰腺腺癌	临床2期	加拿大	Verlyx Pharma, Inc.	2009-01-01
结肠转移性腺癌	临床2期	加拿大	Verlyx Pharma, Inc.	2008-03-01
肝细胞癌	临床1期	加拿大	Verlyx Pharma, Inc.	2014-08-01
心肌梗塞	临床前	美国	Medical College of Wisconsin	2025-04-09

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03403621 (CTgov)	临床1/2期	皮肤增生性瘢痕	6	Pentamidine Isethionate (Topical Pentamidine Isethionate)	範築壓範衊襯網製簾艱 = 艱範鹹蓋醖繭製顧憲艱齋顧窪鬱觸壓製積觸鬱 (齋築膚糧襯鬱衊鏇繭繭, 遞築醖築糧淵鏇鑰餘鹹 ~ 襯積範衊構鏇壓鑰蓋簾) 更多	-	2023-11-22
NCT03403621 (CTgov)	临床1/2期	皮肤增生性瘢痕	6	Placebo (Placebo Control)	範築壓範衊襯網製簾艱 = 鬱窪構夢遞顧遞鑰鹽獵齋顧窪鬱觸壓製積觸鬱 (齋築膚糧襯鬱衊鏇繭繭, 觸餘蓋壓觸夢鬱構壓範 ~ 網獵製餘淵願膚醖衊鬱) 更多	-	2023-11-22
NCT01360762 (CTgov)	临床3期	获得性免疫缺陷综合征 \| 内脏利什曼病	74	Pentamidine	鹹選顧獵築鬱壓膚夢鬱 = 選衊衊範鹽淵獵遞膚醖遞觸築廠積鏇遞醖繭窪 (餘構繭繭齋餘齋鬱範構, 膚醖鹹鹽淵壓構艱窪膚 ~ 範鏇蓋選積窪衊觸獵衊) 更多	-	2019-02-15
NCT02669706 (Pubmed \| Bone Marrow Transplant)	N/A	造血干细胞移植	50	Intravenous pentamidine	簾壓範夢顧遞繭觸艱憲(積窪製簾鑰選觸願遞衊) = 餘憲鏇齋願簾選觸淵廠齋鹹窪選願繭鹹蓋繭廠 (憲糧鹽窪夢壓簾壓淵構 )	-	2018-03-01
NCT01360762 (Pubmed \| Clin Infect Dis)	临床3期	HIV感染 \| 内脏利什曼病	74	Pentamidine secondary prophylaxis	膚襯顧製選鬱鏇鑰網齋(壓願觸鏇願蓋築蓋遞衊) = 構製鹹鹽遞廠艱鏇鏇淵鹹鹹願醖鬱鬱齋鬱製衊 (夢築獵簾夢齋繭鬱遞鹽 ) 更多	-	2018-01-18
Tandem Meetings ASTCT and CIBMTR2017	N/A	血液肿瘤 \| 肺孢子菌肺炎	-	IV Pentamidine	顧遞簾範選積獵廠齋鬱(淵鬱齋糧願簾觸齋選繭) = 餘蓋鹽選衊襯獵觸構鹹壓築範憲夢構選窪願窪 (憲夢淵獵餘窪齋觸觸鹹 ) 更多	-	2017-03-01
NCT00729807 (CTgov)	临床2期	难治性黑色素瘤 \| 皮肤黑色素瘤	6	pentamidine	壓積鬱淵築醖醖鹹網衊 = 繭鏇糧簾餘鹽顧憲網鹹醖淵獵選壓衊蓋網簾膚 (蓋遞鏇鑰遞鏇繭餘蓋醖, 築製築簾餘製夢築糧艱 ~ 遞鬱齋選蓋壓窪鑰鹽憲) 更多	-	2016-10-21
Tandem Meetings ASTCT and CIBMTR2016	N/A	肺孢子菌肺炎 \| 造血干细胞移植	58	Intravenous Pentamidine	夢網製築繭夢齋襯壓製(餘憲齋鏇醖鬱艱蓋窪繭) = 廠製鬱壓鹹壓壓餘襯廠憲網衊襯廠鏇夢齋繭鏇 (襯膚齋艱廠簾選鹽製繭 )	积极	2016-03-01
ARVO2013	N/A	棘阿米巴角膜炎	24	Pentamidine isethionate	鬱網網艱製鬱齋鏇構築(膚鹹遞構鹹鑰築範顧觸) = 餘廠鑰遞構憲選構鑰憲醖願簾齋艱觸網顧壓鹽 (餘壓糧遞衊衊齋餘願壓, 21.7) 更多	-	2013-06-01
NCT00014911 (CTgov)	临床2期	1型糖尿病	36	Islet Transplantation+Ganciclovir+Sulfamethoxazole+Tacrolimus+Sirolimus+Daclizumab+Pentamidine+Trimethoprim	網獵醖蓋醖顧餘壓構顧 = 鹽鑰醖鹽範遞積醖遞壓壓憲膚積鹽網衊艱鑰鏇 (簾廠鏇遞衊網鹽窪壓齋, 鹽餘齋廠艱憲簾製齋遞 ~ 鹽築醖鑰鹽淵淵齋鬱鑰) 更多	-	2012-10-17
NCT00078559 (CTgov)	临床1/2期	肾脏疾病 \| 肾移植排斥反应	10	Kidney transplant+Acyclovir+Acetaminophen+Bactrim+Nystatin+Sirolimus+Clotrimazole+Trimethoprim+Diphenhydramine+TMP+Alemtuzumab+Valgancyclovir+Sulfa+Methylprednisolone+Tacrolimus+Pentamidine	遞觸觸窪醖繭憲壓鏇構 = 構襯蓋餘壓願鑰繭蓋壓築夢鑰製憲繭廠衊製憲 (鏇製蓋蓋壓窪餘齋築鹹, 範鹹壓醖餘夢淵齋鑰憲 ~ 繭鹽窪遞窪顧淵襯製齋) 更多	-	2012-07-09