Delving into the Latest Updates on Pentamidine Isethionate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

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

+ [19]

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious DiseasesRespiratory DiseasesOther Diseases+ [1]

Active Indication

Pneumonia, PneumocystisMyocardial Infarction

Inactive Indication

Advanced Pancreatic AdenocarcinomaHepatocellular CarcinomaMetastatic colon cancer+ [2]

Originator Organization

Fresenius Kabi AG

Active Organization

Medical College of WisconsinSanofi KK

Fresenius Kabi USA LLC

Inactive Organization

Verlyx Pharma, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (16 Oct 1984),

Pneumonia, Pneumocystis

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC23H36N4O10S2

InChIKeyYBVNFKZSMZGRAD-UHFFFAOYSA-N

CAS Registry140-64-7

MAMS4CL comprises a clinical trial with three embedded sub-studies designed to comprehensively evaluate the administered treatments and assess the impact of CL treatment on patients and the healthcare system.
The multi-centre multi-arm multi-stage phase 3 clinical trial is designed to rigorously evaluate a total of 4 alternative treatment options for systemic CL against Sodium Stibugluconate (SSG) as the standard of care. The trial comprises two seamlessly linked stages. In stage 1, all four investigational arms will be evaluated against the control arm for efficacy to inform the selection of the arms, based on a pre-defined efficacy threshold that will advance to stage 2, in addition to the control arm. After stage 2, the experimental interventions will be compared with SSG similar to a standard superiority trial for efficacy. The general study design in stage 1 and stage 2 will be identical; only the number of investigational arms may differ.
Patients will be randomized into the respective treatment arms at the recruitment sites of Arba Minch hospital, Boru Meda hospital and ALERT hospital in Ethiopia. Individuals will be hospitalized during the entire course of their treatment. As different arms have different treatment duration, patient hospitalization period and visit schedules will differ between arms. In total, the study will last 180 days for each participant.

Start Date01 Jan 2027

Sponsor / Collaborator

Armauer Hansen Research Institute

[+4]

NCT07357103

/ Not yet recruitingPhase 4IIT

Positioning Second-line Therapies for Pneumocystis Jirovecii Pneumonia (PCP Alternatives) [A Branch of the Initial Treatment Domain of the SPIRIT-PCP Platform]

The usual first treatment for Pneumocystis jirovecii pneumonia (PCP) is an antibiotic called trimethoprim-sulfamethoxazole (TMP-SMX). However, some patients cannot take this medication because of allergies, side effects, or lack of response.
This study asks the question:
When TMP-SMX cannot be used, which alternative treatment for PCP provides the best balance of effectiveness and safety?

Start Date01 Mar 2026

Sponsor / Collaborator-

NCT03730363

/ CompletedPhase 1IIT

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

Start Date19 Dec 2018

Sponsor / Collaborator

University of Kentucky

100 Clinical Results associated with Pentamidine Isethionate

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100 Translational Medicine associated with Pentamidine Isethionate

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100 Patents (Medical) associated with Pentamidine Isethionate

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3,161

Literatures (Medical) associated with Pentamidine Isethionate

01 May 2026·ENVIRONMENTAL RESEARCH

Multifunctional ultralight Fe3O4/α-Fe/bamboo composites for high-performance microwave absorption, hydrophobicity, and heat response

Article

Author: Li, Neng ; Bao, Minzhen ; Cai, Hanjiang ; Zhang, Weigang ; Yuan, Tiancheng

Developing lightweight, sustainable, and multifunctional electromagnetic wave (EMW) absorbing materials is essential for next-generation electronic devices operating under complex environmental conditions. Herein, a series of ultralight Fe₃O₄/α-Fe/bamboo-derived magnetic carbon composites (MB-600 to MB-900) were fabricated through delignification, precursor impregnation, and in-situ pyrolysis. The hierarchical porous architecture of bamboo, coupled with uniformly distributed magnetic nanoparticles, enables excellent impedance matching and enhances synergistic dielectric, magnetic, and conductive losses. Among the samples, MB-800 exhibits the most remarkable microwave absorption performance, achieving a minimum reflection loss of -71.4 dB at 9.36 GHz with a thin matching thickness of 1.7 mm, and providing an effective absorption bandwidth of 5.76 GHz. Simulation results further confirm that MB-800 significantly reduces monostatic radar cross-section over a wide angular range, demonstrating its strong radar-stealth capability. Moreover, increasing the filler loading boosts electrical conductivity and results in high EMI shielding efficiency dominated by absorption. Benefiting from its highly porous and graphitized carbon-magnetic heterostructure, the composite also exhibits low density (0.47 g/cm³), outstanding hydrophobicity (117.7°), superior thermal safety, and rapid Joule-heating response (151 °C within 10 s at 5 V). This work presents a green and scalable strategy for producing biomass-derived multifunctional magnetic composites, offering promising potential for electromagnetic stealth, EMI shielding, and thermal-management applications.

01 Mar 2026·Journal of Advanced Research

S100B induces angiogenesis via the clathrin/FOXO1/β-catenin signaling pathway and contributes to Bevacizumab resistance in epithelial ovarian cancer

Article

Author: Li, Jun ; Lu, Xin ; Wang, Jieyu ; Xu, Haoya ; Bai, Yang ; Yue, Huiran ; Li, Wenzhi

INTRODUCTION:

Bevacizumab (BEV), the most common antiangiogenic agent for treating ovarian cancer, prolongs progression-free survival (PFS) but does not significantly improve overall survival (OS). Improving the limited clinical benefit of BEV remains a major challenge in ovarian cancer treatment. Although several studies have explored the mechanisms underlying tumor resistance to BEV, the clinical translation of these findings to overcome BEV resistance has been limited.

OBJECTIVES:

To identify the key molecules and mechanisms that modulate ovarian cancer sensitivity to BEV.

METHODS:

RNA sequencing was conducted on BEV-sensitive and BEV-resistant mouse ovarian cancer tissue to identify differentially expressed genes (DEGs). A prognostic assessment was performed and a risk signature was constructed using these DEGs and the BEV-related sequencing datasets. S100B was identified and assessed in angiogenesis using tube formation, 3D fibrin bead sprouting, wound healing, and migration assays. Downstream targets and signaling pathways of S100B in HUVECs were identified by proteomics and validated by western blot. The effect of S100B inhibitors on BEV efficacy was evaluated using in vivo experiments.

RESULTS:

A BEV-related prognostic signature comprising 11 genes was constructed. Of these, S100B expression significantly increased in BEV-resistant mouse ovarian cancer tissue and significantly correlated with poor PFS and OS of ovarian cancer patients treated with a BEV combination chemotherapy. HUVECs co-cultured with S100B-overexpressing ovarian cancer cells promoted tube formation, sprouting, and migration. Exogenous S100B entered HUVECs via clathrin-mediated endocytosis, downregulated FOXO1 expression, and promoted β-catenin nuclear translocation and transcriptional activity, ultimately enhancing tube formation. The S100B inhibitor pentamidine significantly increased BEV responsiveness and prolonged survival in ovarian tumor-bearing mice.

CONCLUSION:

S100B is a key molecule regulating ovarian cancer sensitivity to BEV. Paracrine S100B secreted by ovarian cancer cells acts on HUVECs, promoting angiogenesis through the FOXO1/β-catenin pathway. Pentamidine combined with BEV holds potential for overcoming BEV resistance in clinical use.

01 Feb 2026·CARDIOVASCULAR DRUGS AND THERAPY

Mitigation of Injury from Myocardial Infarction by Pentamidine, an Inhibitor of the Acetyltransferase Tip60

Article

Author: Lough, John W ; Wan, Tina C ; Wang, Xinrui ; Auchampach, John A ; Qu, Zhuocheng ; Harty, Katherine R ; Smith, Brian C

PURPOSE:

There is an urgent unmet need for new pharmacologic approaches that promote re-muscularization and repair following myocardial infarction (MI). We previously reported that genetic depletion of the acetyltransferase Tip60 after MI in a mouse model activates the CM cell-cycle, reduces scarring, and restores cardiac function, and that these beneficial effects are mimicked by the Tip60-selective inhibitor TH1834. Here, we investigated whether the FDA-approved anti-microbial agent pentamidine, a Tip60 inhibitor from which TH1834 is derived, also protects from the damaging effects of MI.

METHODS:

Adult (10-14 weeks old) C57Bl/6 mice were subjected to permanent left coronary artery ligation to induce MI. Subsequently, echocardiography, electrocardiography, cardiac staining, and molecular analyses were performed to monitor the effects of treatment with pentamidine on cardiac injury and function.

RESULTS:

We report that transient systemic administration of pentamidine on days 3-16 post-MI at a daily dose of 3 mg/kg efficiently improved cardiac function for up to ten months. This was accompanied by improved survival, diminished scarring, and increased activation of cell-cycle markers in CMs located in the infarct border zone in the absence of hypertrophy. Histological assessments suggested that post-MI treatment with pentamidine reduced site-specific acetylation of the minor histone variant H2A.Z at lysines K4 and K7 in CMs, indicative of the dedifferentiation process which must occur prior to CM proliferation. Treating mice with pentamidine post-MI produced no prominent electrophysiological changes.

CONCLUSIONS:

These findings support the translational potential of pentamidine for treatment of MI, and provide evidence that functional improvement is mediated, in part, by CM renewal due to inhibition of the acetyltransferase activity of Tip60.

1

News (Medical) associated with Pentamidine Isethionate

07 Mar 2024

·www.businesswire.com

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 .

AACRClinical Result

100 Deals associated with Pentamidine Isethionate

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External Link

KEGG	Wiki	ATC	Drug Bank
D00834	Pentamidine Isethionate	P01CX01	DB00738

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Pneumonia, Pneumocystis	United States	Fresenius Kabi USA LLC	16 Oct 1984

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 2	Poland	Verlyx Pharma, Inc.	01 Sep 2012
Metastatic Colorectal Carcinoma	Phase 2	Canada	Verlyx Pharma, Inc.	01 Mar 2011
Advanced Pancreatic Adenocarcinoma	Phase 2	Canada	Verlyx Pharma, Inc.	01 Jan 2009
Metastatic colon cancer	Phase 2	Canada	Verlyx Pharma, Inc.	01 Mar 2008
Hepatocellular Carcinoma	Phase 1	Canada	Verlyx Pharma, Inc.	01 Aug 2014
Myocardial Infarction	Preclinical	United States	Medical College of Wisconsin	09 Apr 2025

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Tandem Meetings ASTCT and CIBMTR2026	Not Applicable	Hematopoietic stem cell transplantation	1,256	Pentamidine	gblpeqrpet(tgsypuxogf): OR = 2.6 (95.0% CI, 0.17 - 39.43) View more	Positive	04 Feb 2026
Tandem Meetings ASTCT and CIBMTR2026	Not Applicable	Hematopoietic stem cell transplantation	1,256	TMP-SMX		Positive	04 Feb 2026
NCT03403621 (CTgov)	Phase 1/2	Cicatrix, Hypertrophic	6	Pentamidine Isethionate (Topical Pentamidine Isethionate)	jcruyqpqho = rmdaiykywx ogjiqtkzzh (fvgjlwsfzr, oztivefvwo - hbtjfuqeoz) View more	-	22 Nov 2023
NCT03403621 (CTgov)	Phase 1/2	Cicatrix, Hypertrophic	6	Placebo (Placebo Control)	jcruyqpqho = okhwaszvqx ogjiqtkzzh (fvgjlwsfzr, cxftrsarvt - bbumyingcm) View more	-	22 Nov 2023
NCT01360762 (CTgov)	Phase 3	Acquired Immunodeficiency Syndrome \| Leishmaniasis, Visceral	74	Pentamidine	swqszoqjnz = pdfxzxjgfd ecsblbduqo (etbbcxrbhc, efjlabtxad - zziopmsswa) View more	-	15 Feb 2019
NCT02669706 (Pubmed \| Bone Marrow Transplant)	Not Applicable	Hematopoietic stem cell transplantation	50	Intravenous pentamidine	enjwfcggcw(wjisicuzxf) = jabgospbeq xylzaxdoqb (irlpnylbsv )	-	01 Mar 2018
NCT01360762 (Pubmed \| Clin Infect Dis)	Phase 3	HIV Infections \| Leishmaniasis, Visceral	74	Pentamidine secondary prophylaxis	bahvszhucv(ptigbnixze) = ybqggalgtt coxxrxqhss (ieqtqiaedu ) View more	-	18 Jan 2018
Tandem Meetings ASTCT and CIBMTR2017	Not Applicable	Hematologic Neoplasms \| Pneumonia, Pneumocystis	-	IV Pentamidine	njtxxuiapg(brcgqfxjkp) = wfaifeuusu jmlzfqvufz (gdqmwcepzu ) View more	-	01 Mar 2017
NCT00729807 (CTgov)	Phase 2	Refractory Melanoma \| Melanoma, Cutaneous Malignant	6	pentamidine	wotcwblzbe = vwcxzyyxot cgebsrkqfj (iknevzsrbn, glafrdakuw - jrgtjlvqws) View more	-	21 Oct 2016
Tandem Meetings ASTCT and CIBMTR2016	Not Applicable	Pneumonia, Pneumocystis \| Hematopoietic stem cell transplantation	58	Intravenous Pentamidine	wkxlbkthnq(pgdfohzret) = wgomopypjr goguvtgrcf (utsnfdhccc )	Positive	01 Mar 2016
ARVO2013	Not Applicable	Acanthamoeba Keratitis	24	Pentamidine isethionate	iburoxuwif(tmrylvdhju) = tnsrplleqw tszbdjzafc (aqkofvpfhf, 21.7) View more	-	01 Jun 2013
NCT00014911 (Edmonton protocol, CTgov)	Phase 2	Diabetes Mellitus, Type 1	36	Islet Transplantation+Ganciclovir+Sulfamethoxazole+Tacrolimus+Sirolimus+Daclizumab+Pentamidine+Trimethoprim	sjijxpjcfo = kbtovrsbek xvebunhpzs (rtvhwlokxg, vwhmshwpbe - idydqhqowq) View more	-	17 Oct 2012