PDGF inhibitors(Platelet-derived growth factor inhibitors), VEGF-C inhibitors(Vascular endothelial growth factor C inhibitors), Angiogenesis inhibitors

Therapeutic Areas

Congenital DisordersEye DiseasesNeoplasms+ [7]

Active Indication-

Inactive Indication

Choroidal NeovascularizationDiabetic macular oedemaMacular Edema+ [7]

Originator Organization

Genaera Corp.

Active Organization-

Inactive Organization

Ohr Pharmaceutical, Inc.

NeuBase Therapeutics, Inc.Genaera Corp.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

RegulationOrphan Drug (US)

Structure

Molecular FormulaC37H71N3O8S

InChIKeyJMNXSNUXDHHTKQ-QVMSTPCGSA-N

CAS Registry320725-47-1

Clinical Trials associated with Squalamine lactate

ACTRN12619000375156 / CompletedPhase 1

A randomised, controlled phase 1 study to investigate the safety and efficacy of orally administered squalamine in subjects with Motor Neuron Disease

Start Date30 Nov 2017

Sponsor / Collaborator

Wesley Medical Research

NCT02727881 / Unknown statusPhase 3

OHR-1601: A Phase III Study of the Efficacy and Safety of Squalamine Lactate Ophthalmic Solution, 0.2% Twice Daily in Subjects With Neovascular Age-Related Macular Degeneration (AMD)

A Phase 3 Study of the Efficacy and Safety of Squalamine Lactate Ophthalmic Solution 0.2% Twice Daily in Subjects with Neovascular Age-Related Macular Degeneration. Patients will receive injections of ranibizumab. In addition, patients will receive either Squalamine lactate 0.2% eye drops or Placebo eye drops. The study duration is approximately 9 months to primary endpoint

Start Date12 Apr 2016

Sponsor / Collaborator

Ohr Pharmaceutical, Inc.

NCT02511613 / WithdrawnPhase 2

A Study of Safety, Functional and Anatomical Effect of Squalamine Lactate Ophthalmic Solution, 0.2% Administered Twice Daily in Subjects With Neovascular Age-related Macular Degeneration

The purpose of this study is to evaluate anatomical and functional effect of combination therapy of Squalamine Lactate Ophthalmic Solution, 0.2% administered twice daily with monthly ranibizumab intravitreal injections in patients with choroidal neovascularization due to AMD.

Start Date01 Jul 2015

Sponsor / Collaborator

Ohr Pharmaceutical, Inc.

100 Clinical Results associated with Squalamine lactate

100 Translational Medicine associated with Squalamine lactate

100 Patents (Medical) associated with Squalamine lactate

109

Literatures (Medical) associated with Squalamine lactate

01 Jun 2023·Colloids and surfaces. B, Biointerfaces

AFM reveals the interaction and nanoscale effects imposed by squalamine on Staphylococcus epidermidis

Article

Author: EL-Kirat-Chatel, Sofiane ; Beaussart, Audrey ; Brunel, Jean-Michel ; Varbanov, Mihayl ; Salles, Elsa ; Retourney, Chloe ; Risler, Arnaud

The Gram-positive bacterium Staphylococcus epidermidis is responsible for important nosocomial infections. With the continuous emergence of antibiotic-resistant strains, the search for new treatments has been amplified in the last decades. A potential candidate against multidrug-resistant bacteria is squalamine, a natural aminosterol discovered in dogfish sharks. Despite its broad-spectrum efficiency, little is known about squalamine mode of action. Here, we used atomic force microscopy (AFM) imaging to decipher the effect of squalamine on S. epidermidis morphology, revealing the peptidoglycan structure at the bacterial surface after the drug action. Single-molecule force spectroscopy with squalamine-decorated tips shows that squalamine binds to the cell surface via the spermidine motif, most likely through electrostatic interactions between the amine groups of the molecule and the negatively-charged bacterial cell wall. We demonstrated that - although spermidine is sufficient for the initial attachment of squalamine to S. epidermidis - the integrity of the molecule needs to be conserved for its antimicrobial action. A deeper analysis of the AFM force-distance signatures suggests the implication of the accumulation-associated protein (Aap), one of the main adhesins of S. epidermidis, in the initial binding of squalamine to the bacterial cell wall. This work highlights that AFM -combined with microbiological assays at the bacterial suspension scale- is a valuable approach to better understand the molecular mechanisms behind the efficiency of squalamine antibacterial activity.

10 May 2023·International journal of molecular sciences

6-Polyaminosteroid Squalamine Analogues Display Antibacterial Activity against Resistant Pathogens.

Article

Author: Giard, Jean-Christophe ; Desriac, Florie ; Dé, Emmanuelle ; Sichel, François ; Vergoz, Delphine ; Géry, Antoine ; Nilly, Flore ; Barreau, Magalie ; Garon, David ; Chevalier, Sylvie ; Lepetit, Charlie ; Muller, Cécile ; Brunel, Jean Michel ; Jeannot, Katy

A series of 6-polyaminosteroid analogues of squalamine were synthesized with moderate to good yields and evaluated for their in vitro antimicrobial properties against both susceptible and resistant Gram-positive (vancomycin-resistant Enterococcus faecium and methicillin-resistant Staphylococcus aureus) and Gram-negative (carbapenem-resistant Acinetobacter baumannii and Pseudomonas aeruginosa) bacterial strains. Minimum inhibitory concentrations against Gram-positive bacteria ranged from 4 to 16 µg/mL for the most effective compounds, 4k and 4n, and showed an additive or synergistic effect with vancomycin or oxacillin. On the other hand, the derivative 4f, which carries a spermine moiety like that of the natural trodusquemine molecule, was found to be the most active derivative against all the resistant Gram-negative bacteria tested, with an MIC value of 16 µg/mL. Our results suggest that 6-polyaminosteroid analogues of squalamine are interesting candidates for Gram-positive bacterial infection treatments, as well as potent adjuvants to fight Gram-negative bacterial resistance.

27 Oct 2020·Journal of Parkinson's diseaseQ3 · MEDICINE

Squalamine Restores the Function of the Enteric Nervous System in Mouse Models of Parkinson’s Disease

Q3 · MEDICINE

Article

Author: Farhin, Sohana ; Furness, John B. ; Amin, Jessica Y. ; Kunze, Wolfgang A. ; Mao, Yu-Kang ; Stanisz, Andrew M. ; West, Christine L. ; Pustovit, Ruslan ; Barbut, Denise ; Delungahawatta, Thilini ; McQuade, Rachel M. ; Diwakarla, Shanti ; Bienenstock, John ; Zasloff, Michael

Background: Parkinson’s disease (PD) is a progressive neurodegenerative disorder thought to be caused by accumulation of α-synuclein (α-syn) within the brain, autonomic nerves, and the enteric nervous system (ENS). Involvement of the ENS in PD often precedes the onset of the classic motor signs of PD by many years at a time when severe constipation represents a major morbidity. Studies conducted in vitro and in vivo, have shown that squalamine, a zwitterionic amphipathic aminosterol, originally isolated from the liver of the dogfish shark, effectively displaces membrane-bound α-syn. Objective: Here we explore the electrophysiological effect of squalamine on the gastrointestinal (GI) tract of mouse models of PD engineered to express the highly aggregating A53T human α-syn mutant. Methods: GI motility and in vivo response to oral squalamine in PD model mice and controls were assessed using an in vitro tissue motility protocol and via fecal pellet output. Vagal afferent response to squalamine was measured using extracellular mesenteric nerve recordings from the jejunum. Whole cell patch clamp was performed to measure response to squalamine in the myenteric plexus. Results: Squalamine effectively restores disordered colonic motility in vivo and within minutes of local application to the bowel. We show that topical squalamine exposure to intrinsic primary afferent neurons (IPANs) of the ENS rapidly restores excitability. Conclusion: These observations may help to explain how squalamine may promote gut propulsive activity through local effects on IPANs in the ENS, and further support its possible utility in the treatment of constipation in patients with PD.

News (Medical) associated with Squalamine lactate

31 May 2023

·www.biospace.com

Enterin announces FDA acceptance of an investigator sponsored IND to treat a patient with prodromal multisystem atrophy (MSA) with ENT-01

PHILADELPHIA, May 31, 2023 (GLOBE NEWSWIRE) -- Enterin Inc., a privately held, Philadelphia-based, clinical-stage biopharmaceutical company pioneering novel treatments for neurodegenerative and metabolic diseases, announces the acceptance by the U.S. Food and Drug Administration (FDA) of an investigator sponsored Investigational New Drug (IND) application (166532) to treat a patient with prodromal multisystem atrophy (MSA) with ENT-01. Treatment will continue indefinitely or until significant adverse events occur that warrant discontinuation of drug. Individuals diagnosed with MSA have an average life expectancy of 6-8 years and there is no existing treatment which halts the progression of the disease. The condition, an alpha-synucleinopathy similar to Parkinson’s disease, consists of progressive autonomic failure with prominent bowel and bladder symptoms, and central nervous system manifestations include REM-behavior disorder, dysfunctional circadian rhythm, Parkinsonism, and cognitive dysfunction. ENT-01 has been used to treat close to 200 patients with Parkinson’s disease in Phase 2a and Phase 2b (randomized) studies and dose-dependent improvement noted in the symptoms mentioned above ( ). Side effects are largely confined to the GI tract, and consist of nausea, diarrhea, and vomiting. Phase 3 studies in Parkinson’s disease-related constipation and further Phase 2 studies in Parkinson’s disease-related psychosis and dementia are being planned. The patient is a 42-year-old man with a single gene mutation (ATP13A2) which may impair lysosomal clearance mechanisms, and which predisposes to Parkinsonism and MSA. He has a 2-year history of constipation, urinary symptoms, erectile dysfunction, sleep disturbances suggestive of REM-behavior disorder, dysfunctional circadian rhythm and positive alpha-synuclein staining in duodenal enteric neurons. On the basis of these symptoms, he has been diagnosed as having prodromal MSA. ENT-01 (squalamine phosphate) acts locally on enteric neurons and electrostatically displaces misfolded, positively charged proteins such as alpha-synuclein from neuronal membranes, as well as preventing the formation and deposition of alpha-synuclein aggregates. Moreover, in preliminary experiments conducted on the patient’s own cells, ENT-01 completely prevented the oxidative stress response caused by rotenone, a highly toxic agent which impairs mitochondrial function, and which is used in animal models of PD. According to Dr. Denise Barbut, Co-Founder, President and CMO of Enterin, “This is the first time that any compound is being used to prevent the progression of MSA and a milestone in the development of ENT-01 for both treatment and prevention of other neurodegenerative disorders.” Dr. Robert Hauser, the treating physician and Director of the Parkinson’s Disease and Movement Disorders Center of the University of South Florida added, “We hope that ENT-01 will be helpful in preventing progression of MSA in this individual and that this work will help promote personalized medicine for neurodegenerative diseases.” About Enterin Inc. Enterin Inc. is the first company to develop novel compounds that repair the dysfunctional gut-brain axis in patients with neurodegenerative diseases. Enterin Inc. is pioneering the medical community’s understanding of the link between infections, dysfunction of the enteric nervous system (ENS) and the onset and progression of neurodegenerative disease. Enterin’s lead compound, ENT-01, displaces membrane-bound alpha-synuclein (αS) aggregates from nerve cells in the ENS and improves neural signalling between the gut and the brain. Enterin Inc. has completed a large, randomized Phase 2b clinical trial in patients with Parkinson’s disease. The study met all the endpoints. Preparations for Phase 3 studies are currently underway. The second compound, ENT-03, increases insulin sensitivity by acting at the level of the brain. It is being developed for the treatment of diabetes, obesity, and Alzheimer’s disease and Phase 1 clinical trials in subjects with obesity and diabetes will begin in June 2023. For more information, please visit . Enterin Inc: Katherine Wolf k.wolf@enterininc.com Investors: Lee Roth/Julia Weilman Burns McClellan lroth@burnsmc.com/jweilman@burnsmc.com Media: Selina Husain/Robert Flamm, Ph.D. Burns McClellan shusain@burnsmc.com/rflamm@burnsmc.com

Phase 2Clinical ResultPhase 1

02 Dec 2014

·www.biospace.com

Ohr Pharmaceutical To Present At The Oppenheimer 25th Annual Healthcare Conference

NEW YORK, Dec. 2, 2014 (GLOBE NEWSWIRE) -- Ohr Pharmaceutical, Inc. (Nasdaq:OHRP), an ophthalmology research and development company, today announced that Dr. Irach Taraporewala, Chief Executive Officer, will present a corporate overview and business update at the Oppenheimer & Co., Inc.'s 25th Annual Healthcare Conference, being held at the Crowne Plaza Hotel in New York City on December 10-11, 2014. Details of the presentation: Date: Thursday, December 11 Time: 3:20pm Eastern Webcast: About Ohr Pharmaceutical, Inc. Ohr Pharmaceutical, Inc. (OHRP) is an ophthalmology research and development company. The company's lead product, Squalamine, is currently being studied as an eye drop formulation in several company sponsored and investigator sponsored Phase II clinical trials for various back-of-the-eye diseases, including the wet form of age-related macular degeneration, retinal vein occlusion, diabetic macular edema, and proliferative diabetic retinopathy. In addition, Ohr has a sustained release micro fabricated micro-particle ocular drug delivery platform with several preclinical drug product candidates in development for glaucoma, steroid-induced glaucoma, ocular allergies, and protein drug delivery. The lead sustained release program in glaucoma is proceeding under a collaboration with a large global pharmaceutical company. Additional information on the company may be found at . CONTACT: Ohr Pharmaceutical Inc. Investor Relations 888-388-2327 ir@ohrpharmaceutical.com LifeSci Advisors, LLC Michael Wood 646-597-6983 mwood@lifesciadvisors.com Help employers find you! Check out all the jobs and post your resume.

19 Jun 2007

·www.biospace.com

Genaera Corporation to Present Preclinical Data on Trodusquemine for the Treatment of Obesity at the American Diabetes Association 67th Scientific Sessions

PLYMOUTH MEETING, Pa., June 19 /PRNewswire-FirstCall/ -- Genaera Corporation today announced that it will present a poster on trodusquemine (MSI-1436), its novel anti-obesity compound, during the American Diabetes Association (ADA) 67th Scientific Sessions, June 22 to 25 in Chicago. The abstract, # 1801-P, is titled, "Trodusquemine is a Multiple Pathway Inhibitor that Causes Differential Weight Loss, Reduces Adiposity, and Improves Plasma Insulin and Leptin Levels." The poster will be available from Saturday, June 23 through Monday, June 25 during the times the General Poster Session is open to conference attendees. Representatives from Genaera will be available to discuss the poster on Sunday, June 24 from 6:15 p.m. to 7:30 p.m. (CT) and on Monday, June 25 from 12:00 p.m. to 2:00 p.m. (CT). For more information online, please visit: uID=1000 About Trodusquemine (MSI-1436) Trodusquemine is a centrally and peripherally-acting appetite suppressant and the first highly selective inhibitor of protein tyrosine phosphatase 1B (PTP-1B). PTP-1B is central to controlling the function of both the leptin and insulin pathways. By inhibiting PTP-1B, MSI-1436 is expected to decrease appetite and normalize blood sugar. Trodusquemine has produced consistent, sustainable weight loss in a variety of animal models and appears to overcome metabolic readjustment, which often limits sustained weight loss during caloric restriction. In addition, trodusquemine has shown the ability to reverse co-morbidities associated with obesity such as abnormal glucose metabolism and cholesterol elevation. About Genaera Genaera Corporation is focused on advancing the science and treatment of metabolic diseases. The Company has significant market opportunities with a first-in-class molecule, trodusquemine (or MSI-1436), that has the potential to redefine the treatment paradigm for obesity and type 2 diabetes and is presently in a Phase 1 trial in obesity. In addition, Genaera has a value-driven, fully out-licensed partnership with MedImmune for a second core program that is presently undergoing Phase 2 clinical testing in asthma. Genaera is committed to directing resources to its core program and the aggressive clinical development of its key assets to build stockholder value. . This announcement contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 that are subject to risks and uncertainties, known and unknown. Forward-looking statements reflect management's current views and are based on certain expectations and assumptions. Such statements include, among others, statements regarding these preliminary results, clinical development plans and prospects for Genaera's programs including trodusquemine (MSI-1436), the IL-9 antibody program, LOMUCIN(TM), or squalamine. You may identify some of these forward-looking statements by the use of words in the statements such as "anticipate," "believe," "continue," "develop," "expect," "plan" and "potential" or other words of similar meaning. Genaera's actual results and performance could differ materially from those currently anticipated and expressed in these and other forward-looking statements as a result of a number of risk factors, including, but not limited to: Genaera's history of operating losses since inception and its need for additional funds to operate its business; the costs, delays and uncertainties inherent in scientific research, drug development, clinical trials and the regulatory approval process; the risk that clinical trials for Genaera's product candidates, including trodusquemine (MSI-1436), the IL-9 antibody program, LOMUCIN(TM), or squalamine may be delayed or may not be successful; the risk that Genaera may not obtain regulatory approval for its products, whether due to adequacy of the development program, the conduct of the clinical trials, changing regulatory requirements, different methods of evaluating and interpreting data, regulatory interpretations of clinical risk and benefit, or otherwise; Genaera's reliance on its collaborators, in connection with the development and commercialization of Genaera's product candidates; market acceptance of Genaera's products, if regulatory approval is achieved; competition; general financial, economic, regulatory and political conditions affecting the biotechnology and pharmaceutical industry; and the other risks and uncertainties discussed in this announcement and in Genaera's filings with the U.S. Securities and Exchange Commission, all of which are available from the Commission in its EDGAR database at as well as other sources. You are encouraged to read these reports. Given the uncertainties affecting development stage pharmaceutical companies, you are cautioned not to place undue reliance on any such forward-looking statements, any of which may turn out to be wrong due to inaccurate assumptions, unknown risks, uncertainties or other factors. Genaera does not intend (and it is not obligated) to publicly update, revise or correct these forward-looking statements or the risk factors that may relate thereto. Genaera Corporation CONTACT: investor relations, Genaera Corporation, +1-610-941-5675; ormedia, Susan Neath of Porter Novelli Life Sciences, +1-619-849-6007,sneath@pnlifesciences.com Web site:

AntibodyFirst in ClassCollaborate

100 Deals associated with Squalamine lactate

External Link

KEGG	Wiki	ATC	Drug Bank
D05914	Squalamine lactate	-	DB06461

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Choroidal Neovascularization	Phase 3	US	Genaera Corp.	01 Jun 2005
Wet age-related macular degeneration	Phase 3	US	Genaera Corp.	01 Jun 2005
Wet Macular Degeneration	Phase 3	US	Genaera Corp.	01 Jun 2005
Macular Edema	Phase 2	-	Ohr Pharmaceutical, Inc.	01 Apr 2013
Retinal Vein Occlusion	Phase 2	-	Ohr Pharmaceutical, Inc.	01 Apr 2013
Diabetic macular oedema	Phase 2	US	NeuBase Therapeutics, Inc.	-
Non-Small Cell Lung Cancer	Phase 2	US	Genaera Corp.	-
Ovarian Cancer	Phase 2	US	NeuBase Therapeutics, Inc.	-
Prostatic Cancer	Phase 2	US	Genaera Corp.	-
Myositis Ossificans	Phase 1	US	Genaera Corp.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02727881 (MAKO, PipelineReview) Manual	Phase 3	Wet Macular Degeneration	237	Ranibizumab+squalamine	wauelydmju(ovcqcxpnkm) = sekecsgzjh zfecejxzla (xhtvwjuikd )	Negative	05 Jan 2018
				Ranibizumab+Placebo	wauelydmju(ovcqcxpnkm) = eeeuzycnsz zfecejxzla (xhtvwjuikd )
ARVO2005	Phase 2	Age Related Macular Degeneration	-	Squalamine lactate 40 mg	agqkefzjcs(xiooitmqpu) = There were no serious adverse events related to study drug reported. A small number of patients reported injection site pain, but no patients withdrew due to adverse events xnvuwjcuqz (tnaylxjsli ) View more	-	01 May 2005
				Squalamine lactate 20 mg
ASCO2004	Phase 2	Advanced Lung Non-Small Cell Carcinoma First line	45	Squalamine 100 mg/m2	uphapxqowh(ghvjcjrute) = ybixrnfbzr tiqotzrbua (pxyppvdmlh ) View more	Negative	15 Jul 2004
				Squalamine 200 mg/m2	uphapxqowh(ghvjcjrute) = pwdjzmrqkd tiqotzrbua (pxyppvdmlh ) View more

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