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- || razuprotafib topical (AKB-9778 topical) / Aadi Biosci
Clinical, Journal: Tie2 Activation via VE-PTP Inhibition With Razuprotafib as an Adjunct to Latanoprost in Patients With Open Angle Glaucoma or Ocular Hypertension. (Pubmed Central) - Jan 27, 2022
Topical ocular razuprotafib as an adjunct to latanoprost therapy was well tolerated and significantly reduced IOP in patients with OAG/OHT. These data support the IOP lowering efficacy of targeting Tie2 activation in Schlemm's canal in the relevant patient population.
- | razuprotafib topical (AKB-9778 topical) / Aerpio, razuprotafib subcutaneous (AKB-9778 SC) / Aerpio
Journal: A Small Molecule Inhibitor of VE-PTP Activates Tie2 in Schlemm's Canal Increasing Outflow Facility and Reducing Intraocular Pressure. (Pubmed Central) - May 13, 2021
This is the first report of IOP lowering in humans with a Tie2 activator and functional demonstration of its action in remodeling SC to increase outflow facility and lower IOP in fully developed mice. Based on these studies, a phase II clinical trial is in progress to advance topical ocular AKB-9778 as a first in class, Tie2 activator for treatment for ocular hypertension and glaucoma.
- ||| razuprotafib topical (AKB-9778 topical) / Aadi Biosci
Trial completion: Study to Assess the Efficacy, Safety and Tolerability of AKB-9778 Ophthalmic Solution as and Adjunct to Latanoprost in Patients With Ocular Hypertension or Open Angle Glaucoma (clinicaltrials.gov) - Jan 14, 2021
P2, N=194, Completed, Sponsor: Aerpio Therapeutics
Based on these studies, a phase II clinical trial is in progress to advance topical ocular AKB-9778 as a first in class, Tie2 activator for treatment for ocular hypertension and glaucoma. Recruiting --> Completed
- | razuprotafib (AKB-9778) / Aerpio
Journal: The VE-PTP Inhibitor AKB-9778 Improves Antitumor Activity and Diminishes the Toxicity of Interleukin 2 (IL-2) Administration. (Pubmed Central) - Jun 19, 2020
The findings suggest that AKB-9778 may function through reducing serum angiopoietin 2 level and regulating EC viability. These findings provide insights into the targeting VE-PTP to improve tolerance and efficacy of IL-2 therapy and highlight the clinical potential of AKB-9778 for treating patients with VLS and cancer.
- ||| razuprotafib topical (AKB-9778 topical) / Aadi Biosci
Enrollment open: Study to Assess the Efficacy, Safety and Tolerability of AKB-9778 Ophthalmic Solution as and Adjunct to Latanoprost in Patients With Ocular Hypertension or Open Angle Glaucoma (clinicaltrials.gov) - Jun 11, 2020
P2, N=195, Recruiting, Sponsor: Aerpio Therapeutics
These findings provide insights into the targeting VE-PTP to improve tolerance and efficacy of IL-2 therapy and highlight the clinical potential of AKB-9778 for treating patients with VLS and cancer. Not yet recruiting --> Recruiting
- |||| razuprotafib topical (AKB-9778 topical) / Aadi Biosci
New P2 trial: Study to Assess the Efficacy, Safety and Tolerability of AKB-9778 Ophthalmic Solution as and Adjunct to Latanoprost in Patients With Ocular Hypertension or Open Angle Glaucoma (clinicaltrials.gov) - May 27, 2020
P2, N=195, Not yet recruiting, Sponsor: Aerpio Therapeutics
- razuprotafib (AKB-9778) / Aerpio
Predictive Value of ERG, OCT-A, and UWF-FA in Patients with Diabetic Retinopathy (Ballroom I) - Mar 9, 2020 - Abstract #ARVO2020ARVO_4709;
Purpose To assess the value of electroretinography (ERG), OCT-angiography (OCT-A), and ultra-wide field fluorescein angiography (UWF-FA) parameters to predict progression of diabetic retinopathy in eyes with moderate to severe non-proliferative diabetic retinopathy (NPDR).Methods In the TIME-2b trial 167 patients with NPDR were randomized to receive 48 weeks of treatment with AKB-9778 (a Tie2 activator) 15 mg once or twice daily, or placebo...Pre-treatment ERG and OCT-A parameters were better predictors of progression to DME/PDR than DRSS or UWF-FA over 48-weeks of follow-up. The combination of functional and structural measures was better than either alone.
- | nesvacumab (REGN910) / Regeneron, Lucentis (ranibizumab) / Roche, Novartis
Review, Journal: Tie-2/Angiopoietin pathway modulation as a therapeutic strategy for retinal disease. (Pubmed Central) - Oct 27, 2019
AKB-9778 is a subcutaneously administered VE-PTP inhibitor that, when combined with monthly ranibizumab, reduced DME more effectively than ranibizumab monotherapy in a phase 2 study...AXT107, currently in the preclinical phase, promotes conversion of Ang-2 into a Tie-2 agonist and blocks signaling through VEGFR2 and other receptor tyrosine-kinases. Expert Opinion: Tie-2/Angiopoietin pathway modulators show promise to reduce treatment burden and improve visual outcomes in nAMD and DME, with potential to treat cases refractory to current treatment modalities.