Evizon (squalamine) / NeuBase Therap - LARVOL DELTA

Evaluation of Cytotoxicity and α-Glucosidase Inhibitory Activity of Amide and Polyamino-Derivatives of Lupane Triterpenoids. (PubMed, Molecules) - "The betulonic acid diethylentriamine conjugate showed partial activity against methicillin-resistant S. aureus and the fungi C. neoformans. These results show that triterpenic polyamines, being analogs of steroidal squalamine and trodusquemine, are important substances for the search of new drugs with anticancer, antidiabetic, and antimicrobial activities."

Journal • Oncology

New Gnamptodontinae (Hymenoptera: Braconidae) from China and Vietnam, with two genera new for China and seven new species. (PubMed, Zootaxa) - "from China (Yunnan), Tamdaona brevizona van Achterberg, sp...n.) and Alysdacnusa atomus (Papp, 2004) is a new combination (comb. n.)."

Journal

Squalamine Restores the Function of the Enteric Nervous System in Mouse Models of Parkinson's Disease. (PubMed, J Parkinsons Dis) - "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."

Journal • Preclinical • CNS Disorders • Constipation • Gastroenterology • Gastrointestinal Disorder • Movement Disorders • Parkinson's Disease

Squalamine and Aminosterol Mimics Inhibit the Peptidoglycan Glycosyltransferase Activity of PBP1b. (PubMed, Antibiotics (Basel)) - "In this work, we report that the aminosterol squalamine and mimic compounds present an unexpected mode of action consisting in the inhibition of the GTase activity of the model enzyme PBP1b. In addition, selected compounds were able to specifically displace the lipid II from the active site in a fluorescence anisotropy assay, suggesting that they act as competitive inhibitors."

Journal

Recent Innovations in Medical and Surgical Retina. (PubMed) - "Several treatment approaches are effective in the treatment of diabetic macular edema. Prophylaxis against AMD progression with Age-Related Eye Disease Study-2 supplements seems to reduce the risk of developing neovascular but not atrophic complications of AMD. Enhanced-depth imaging optical coherence tomography data provide new information on the role of the choroid in a variety of conditions. Advances in gene- and cell-based therapy will revolutionize the development of regenerative medicine in ophthalmology."

Journal • Biosimilar • Diabetes

Ohr Pharma: Annual Report 2015 (Ohr Pharmaceutical) - Anticipated additional data presentation from P2 IMPACT study (NCT01678963) for wet AMD at a scientific conference in 2016; Anticipated initiation of P3 trial for wet AMD in Q1 2016; Anticipated data from P2 OHR-1501 study (NCT02511613) of squalamine lactate in combination with Lucentis for neovascular AMD in 2016

Anticipated new P3 trial • Anticipated P2 data • Ophthalmology

Ohr Pharmaceutical provides update on ongoing squalamine clinical trial in wet-AMD (Ohr Pharmaceutical Press Release) - P3, N=200; NCT02727881; "Ohr Pharmaceutical...announced that it plans to amend the ongoing clinical trial investigating Squalamine in wet-AMD (the MAKO Study) to enable efficacy analyses by the end of calendar 2017 or early 2018...Company Now Fully Funded Through Efficacy Data From Ongoing Trial and Into 2018."

Financing • P3 data • Age-related Macular Degeneration • Ophthalmology

Ohr Pharmaceutical reports fiscal first quarter 2018 financial results (Ohr Pharmaceutical Press Release) - "The MAKO study evaluated the efficacy and safety of topically administered squalamine in combination with monthly Lucentis...for the treatment of wet age-related macular degeneration...Based on the results, the Company has discontinued further development of squalamine and is evaluating strategic alternatives."

Discontinued • Age-related Macular Degeneration • Ophthalmology

Ohr Pharmaceutical, Inc. announces enrollment of first patient in phase III wet AMD clinical program (GlobeNewswire) - P3, N=650; NCT02727881; Sponsor: Ohr Pharmaceutical; "Ohr Pharmaceutical...today announced that the first patient has been enrolled in the first Phase III clinical trial of...squalamine lactate ophthalmic solution...for the treatment of neovascular age-related macular degeneration..."

Enrollment open • Age-related Macular Degeneration • Ophthalmology

OHR Pharma: ARVO 2016 (Ohr Pharmaceutical) - "The post hoc analyses of lesion characteristics as predictive factors of visual outcome in the IMPACT data revealed that combination therapy with Squalamine was most effective in those subjects whose occult component was smaller than 10 mm². This effect was not seen in the ranibizumab alone arm"

P2 data • Age-related Macular Degeneration • Ophthalmology

Ohr Pharmaceutical, Inc. announces SPA agreement with US FDA and initiation of phase III wet AMD clinical program (Ohr Pharmaceutical Press Release) - "Ohr Pharmaceutical...today announced that it has reached an agreement on the Special Protocol Assessment (SPA) with the United States Food and Drug Administration (US FDA) on the design of the Phase III trial for...squalamine lactate ophthalmic solution, 0.2%...Ohr has initiated the first of two planned Phase III global clinical studies evaluating the efficacy and safety of Squalamine, given in combination with Lucentis®, for the treatment of neovascular age-related macular degeneration..."

New P3 trial • Special Protocol Assessment • Age-related Macular Degeneration • Ophthalmology

Squalamine: "Better Final VA with Squalamine Combination Therapy" (Ohr Pharmaceutical) - Dawson James Securities 3rd Annual Small Cap Growth Conference 2017

P2 data • Age-related Macular Degeneration • Ophthalmology

Ohr Pharmaceutical announces efficacy results from the MAKO study in wet-AMD (Ohr Pharmaceutical Press Release) - P3, N=200; NCT02727881; Sponsor: Ohr Pharmaceutical; "Ohr Pharmaceutical...today reported topline data from the MAKO study which did not meet its primary efficacy endpoint...Subjects receiving squalamine combination therapy (n=119) achieved a mean gain of 8.33 letters from baseline versus 10.58 letters from baseline with Lucentis® monotherapy (n=118). There were no differences in the safety profile between the two treatment groups."

P3 data: top line • Age-related Macular Degeneration • Ophthalmology

Study on Synthesis of Key Squalamine intermediate 7α, 24R -Dihydroxy-5α-cholestan-3-one. (PubMed, Steroids) - "A facile novel strategy has been developed to obtain a key intermediate of squalamine, 7α, 24R -dihydroxy-5α-cholestan-3-one, starting from methyl Δ-3β-hydroxycholanate. The pure product was successfully synthesized and separated from the C-24 position epimers in good purity, d.e.% and yield."

Journal

SQUALAMINE, AN AMINOSTEROL POTENTIALLY USEFUL IN TREATING PARKINSON’S DISEASE, ACTIVATES THE AFFERENT VAGUS NERVE VIA ACTION ON THE ENTERIC NERVOUS SYSTEM (DDW 2020) - "The excitatory response of vagal fibres to squalamine was reduced by about 50% following synaptic blockade within the myenteric plexus. These results suggest that the excitatory effect of squalamine on the vagus is mediated by neurotransmission via intramural sensory synapses."

Staphylococcus aureus nasal decolonization strategies: a review. (PubMed, Expert Rev Anti Infect Ther) - "Areas covered: Mupirocin nasal ointment has been used for the nasal decolonization and prevention of staphylococcal infections in various settings like surgeries...Some old approved antiseptics (chlorhexidine, povidone-iodine) or antibiotics (rifampicin, bacitracin) have been investigated for their efficacy in this indication. Other new agents (tea tree oil, retapamulin, LTX-109, XF-73, phages, lysostaphin, squalamine analogues, etc.) are being studied. Some of them are still in preclinical phases, and others have reached clinical trials, but further research is needed. Special interest should be given to single dose decolonization strategies and to molecules that do not select resistant strains."

Journal

Innovative therapies for neovascular age-related macular degeneration. (PubMed, Expert Opin Pharmacother) - "Expert opinion: Long-acting anti-VEGF agents have demonstrated promising results in phase 3 studies, and include Brolucizumab, a single-chain antibody fragment, and Abicipar, a designed ankyrin repeat protein (DARPin). Other unique anti-VEGF agents in current trials include Conbercept - a fusion protein of the VEGF receptor domains, KSI-301 - an anti-VEGF antibody biopolymer conjugate, and OPT-302 - an inhibitor of VEGF-C/D. Strategies to activate the Tie-2 receptor, some in combination with VEGF inhibition, are of interest, with recent trials of Faricimab, ARP-1536, and nesvacumab. Topical anti-VEGF ± anti-PDGF agents, such as pazopanib, squalamine lactate, regorafenib, and LHA510 have shown limited efficacy and/or have not been advanced, although PAN-90806 continues to advance with promising initial results. Sustained-release anti-VEGF treatments, to address treatment burden, include the ranibizumab Port Delivery System, GB-102, NT-503, hydrogel depot,..."

Journal

Squalamine blocks tumor-associated angiogenesis and growth of human breast cancer cells with or without HER-2/neu overexpression. (PubMed, Cancer Lett) - "Overexpression of HER-2/neu receptors occur in 25-30% of breast cancers, and treatment with trastuzumab inhibits HER-2-overexpressing tumor growth. These effects correlated with blockade of focal adhesion kinase phosphorylation and stress fiber assembly in HUVECs. Thus, squalamine effectively inhibits growth of breast cancers with or without HER-2-overexpression, an effect due in part to blockade of tumor-associated angiogenesis."

Journal

A squalamine derivative, NV669, as a novel PTP1B inhibitor: in vitro and in vivo effects on pancreatic and hepatic tumor growth. (PubMed, Oncotarget) - "Subsequently, our in vivo results showed that NV669 inhibited the growth of pancreatic and hepatic tumor xenografts with a significant cell cycle arrest in pre-mitotic phase and an increase of tumor cell apoptosis. Therefore, NV669 may serve as an alternative anticancer agent, used alone or in association with other medications, for the treatment of pancreatic adenocarcinoma and hepatocellular carcinoma."

Journal • Preclinical • CASP8 • CCNB1 • CDH1 • CDK1 • PARP

Colonic Motility and Jejunal Vagal Afferent Firing Rates Are Decreased in Aged Adult Male Mice and Can Be Restored by an Aminosterol. (PubMed, Front Neurosci) - "Our results show for the first time that the jejunal vagal afferent firing rate is reduced in aged-mice. They also suggest that there is translational potential for the therapeutic use of squalamine in the treatment of age-related constipation and dysmotility."

Journal

Anti-persister activity of squalamine against Acinetobacter baumannii. (PubMed, Int J Antimicrob Agents) - "Squalamine did not induce persisters nor VBNCs formation in A. baumannii ATCC 17978. Interestingly, it was significantly active against this type of dormant population generated by ciprofloxacin, making it a very promising anti-persister agent."

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