AMA0076 / Amakem, Akari Therap - LARVOL DELTA

Identifying new drugs and targets to treat rapidly elevated intraocular pressure for angle closure and secondary glaucomas to curb visual impairment. (PubMed, Exp Eye Res) - "However, translation of the novel animal-based findings to the human conditions remains to be demonstrated but represent viable targets, especially EP-receptor agonists (e.g. omidenepag isopropyl; AL-6598; butaprost), mixed activity serotonin/dopamine receptor agonists (e.g. cabergoline), rho kinase inhibitors (e.g. AMA0076, Y39983), CACNA2D1-gene product inhibitors (e.g. pregabalin), melatonin receptor agonists, and certain K-channel openers (e.g. nicorandil, pinacidil). Other drug candidates and targets were also identified and will be discussed."

Journal • Review • Cardiovascular • Glaucoma • Infectious Disease • Ocular Inflammation • Ophthalmology

Novel ROCK Inhibitors, Sovesudil and PHP-0961, Enhance Proliferation, Adhesion and Migration of Corneal Endothelial Cells. (PubMed, Int J Mol Sci) - "In all experiments, sovesudil and PHP-0961, the novel ROCK inhibitors, were equal or superior to the results of the ROCK inhibitor positive control, Y-27632. In conclusion, sovesudil and PHP-0961, novel ROCK inhibitors have the capacity to regenerate hCEnCs by enhancing cell proliferation and adhesion between cells."

Journal • Ophthalmology • Transplantation • CTNNB1 • SOX2 • TJP1

Novel ROCK Inhibitors on the Regeneration of Corneal Endothelial Cells (ARVO 2022) - "Novel ROCK inhibitors have a capacity to regenerate HCEnCs through enhancing the cell proliferation and adhesion between cells."

Ophthalmology • SOX2 • TJP1

Sovesudil (locally acting rho kinase inhibitor) for the treatment of normal-tension glaucoma: the randomized phase II study. (PubMed, Acta Ophthalmol) - "Sovesudil 0.25% and 0.5% TID showed statistically significant IOP-lowering effects and 0.5% concentration's IOP-lowering effects met the superiority criteria in comparison with the placebo at week 4. Sovesudil was well tolerated with mild adverse events including relatively low incidence of conjunctival hyperaemia in patients with NTG."

Clinical • Journal • P2 data • Glaucoma • Ophthalmology

A Study of Efficacy and Safety of PHP-201 in Patients With Primary Open Angle Glaucoma or Ocular Hypertension (clinicaltrials.gov) - P3; N=110; Not yet recruiting; Sponsor: pH Pharma; Trial completion date: Nov 2025 ➔ Nov 2023

Trial completion date • Glaucoma • Ophthalmology

Rho-kinase (ROCK) Inhibitors- A Neuroprotective Therapeutic Paradigm with a Focus on Ocular Utility. (PubMed, Curr Med Chem) - "Based on the results of high-throughput screening, several Rho kinase inhibitors have been designed and developed comprising of diverse scaffolds exhibiting Rho kinase inhibitory activity from micromolar to subnanomolar ranges. This diversity in the scaffolds with inhibitory potential against the kinase and their SAR development will be intricated in the present review. Ripasudil is the only Rho kinase inhibitor marketed to date for the treatment of glaucoma. Another ROCK inhibitor AR-13324 has recently passed the clinical trials whereas AMA0076, K115, PG324, Y39983 and RKI-983 are still under trials. In view of this, a detailed and updated account of ROCK II inhibitors as the next generation therapeutic agents for glaucoma will be discussed in this review."

Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Complement-mediated Rare Disorders • Gene Therapies • Glaucoma • Hypertension • Ischemic stroke • Multiple Sclerosis • Myocardial Ischemia • Nephrology • Ocular Inflammation • Ophthalmology • Optic Neuritis • Orthopedics • Pain • Renal Disease • Reperfusion Injury