Table 3.
Current Investigational Pharmacotherapy for Diabetic Retinopathy and Diabetic Macular Edema(1–4)
| Pharmacological Agent | Mechanism Category | Administration Route | Trial Phase | Sponsor |
|---|---|---|---|---|
| Abicipar pegol | DARPin | IVit | II | Allergan |
| AKB-9778 | Tie2 agonist | SC | II | Aerpio Therapeutics |
| ALG-1001 | Integrin receptor antagonist | IVit | II | Allegro Ophthalmics |
| Alpha lipoic acid | Antioxidant | PO | III | Ludwig-Maximilians University of Munich |
| Aminoguanidine | AGE Inhibitor | PO | I | University of Minnesota |
| AR-13503 | Rho kinase & Protein kinase C inhibitor | IVit | I | Aerie Pharmaceuticals |
| ASP8232 | Vascular adhesion protein 1 inhibitor | PO | II | Astellas Pharma |
| Bevasiranib (Cand5) | siRNA silencing of VEGF mRNA | IVit | II | Opko Health, Inc. |
| Betamethasone (DE-102) | Corticosteroid | ST | III | Santen Pharmaceutical Co. |
| BI 1026706 | Bradykinin 1 Antagonist | PO | II | Boehringer Ingelheim |
| BI 1467335 | SSAO (VAP-1) Inhibitor | PO | IIa | Boehringer Ingelheim |
| Brimonidine | Neuroprotection | Top | III | European Consortium for the Early Treatment of Diabetic Retinopathy (EUROCONDOR) |
| Brolucizumab | Anti-VEGF | IVit | III | Novartis Pharmaceuticals |
| Bromocriptine, | Dopaminergic | PO | I/II | University of Southern California |
| Candesartan | Angiotensin receptor blocker | PO | III | AstraZeneca |
| Celecoxib | COX-2 inhibitor | Top | I | University of Coimbra |
| Choline fenofibrate | Triglyceride reduction | PO | II | Abbott |
| Conbercept | Anti-VEGF Anti-PlGF |
IVit | III | Chengdu Kanghong Biotech Co |
| Danazol | Androgenic vascular permeability modulator | PO | II/III | Ampio Pharmaceuticals |
| Darapladib | Phospholipase CA2 inhibitor | PO | II | GlaxoSmithKline |
| Dextromethorphan | NMDA receptor antagonism, insulinogenic | PO | II | NEI |
| Diclofenac | NSAID | IVit | IIa | Shahid Beheshti University of Medical Sciences |
| Doxycycline | Anti-inflammatory | PO | I/II | NEI |
| DS-7080a | Anti-angiogenic mAb | IVit | I/II | Daiichi Sankyo, Inc. |
| EBI-031 | Anti-interleukin-6 antibody | IVit | I | Eleven Biotherapeutics (Sesen Bio) |
| Emixustat | RPE65 inhibition | PO | II | Acucela Inc. |
| Empagliflozin | SGLT2 inhibitor | PO | IV | Hannover Medical School |
| Faricimab | Anti-VEGF & Ang-2 inhibitor | IVit | II | Roche/Genentech |
| Fasudil | Rho-kinase inhibitor | IVit | II | Shahid Beheshti University of Medical Sciences |
| Fenofibrate | PPARalpha agonist | PO | IV | University of Padova |
| Folic acid, B6, B12 | Antioxidant | PO | IV | University of Catania |
| FOV2304 | Kinin β1 receptor Antagonist (anti-angiogenic) | Top | II | Fovea Pharmaceuticals |
| GB-102 | pan-VEGF inhibitor | IVit | IIa | Graybug Vision |
| iCo-007 | Anti-sense c-RAFkinase | IVit | II | iCo Therapeutics |
| Infliximab | Anti-TNF alpha mAb | IVit | I | Retina Research Foundation |
| Ketorolac | NSAID (coxib) | Top | I | Roche |
| KP-121 | Corticosteroid | Top | II | Kala Pharmaceuticals |
| KSI-301 | Anti-VEGF Biopolymer | IVit | Ib | Kodiak Sciences |
| KVD001 | Plasma kallikrein inhibitor | IVit | II | Kalvista Pharmaceuticals |
| Levosulpiride | Dopamine D2 receptor blocker | PO | III | National University of Mexico (UNAM) |
| LKA651 | Anti-erythropoietin | IVit | I | Novartis |
| Luminate (Risuteganib) | Integrin receptor antagonist | IVit | III | Allegro Ophthalmics |
| Mecamylamine | nACh antagonist | Top | II | CoMentis |
| Minocycline | Anti-microglial (anti-inflammatory) | PO | III | NEI |
| MTP-131 | Mitochondrial cardiolipin promoter | Top | I/II | Stealth Biotherapeutics |
| Nutritional supplements | Anti-oxidative stress | PO | II | Mid-Atlantic Retinal Consultants |
| Ocriplasmin | PVD Induction | IVit | I | ThromboGenics |
| Octreotide | GH inhibitor | SC | III | Novartis |
| OC-10X | Tubulin inhibitor | Top | I | OcuCure Therapeutics |
| Opt-302 | VEGF-r/Fc-fusion | IVit | II | Opthea |
| PAN-90806 | VEGF2R tyrosine kinase inhibitor | Top | II | PanOptica |
| Pemafibrate | PPARalpha agonist | PO | III | Jaeb Center for Health Research |
| PF-04523655 | siRNA against RTP801 (antiangiogenic) | IVit | II | Quark Pharmaceuticals |
| REGN910-3 (nesvacumab) | Anti-angiopoietin 2 mAb | IVit | II | Regeneron/Bayer |
| RO6867461 | bi-specific anti-VEGF/antiangiopoietin 2 | IVit | II | Hoffman-LaRoche |
| Ruboxistaurin | PKC-β inhibitor | PO | III | Chromaderm, Inc. & Eli Lilly & Co |
| SF0166 | alphaVbeta3 integrin inhibitor | Top | I/II | SciFluor |
| Sirolimus | Anti-IL-2 (mTOR inhibitor) |
IVit/SConj | II | Santen Pharmaceutical & NEI |
| Somatostatin | Neuroprotection | Top | III | European Consortium for the Early Treatment of Diabetic Retinopathy (EUROCONDOR) |
| Sorbinil | Aldose Reductase inhibitor |
PO | III | NEI |
| Squalamine | Anti-angiogenic | Top | II | Elman Retina Group |
| Sulodexide | Glycosaminoglycan analogue | PO | II | DRESS Research Group |
| Teprotumumab | IGF-1 receptor antagonist | IV | I | River Vision Development Corporation |
| TG100801 | Anti-angiogenic | Top | I | TargeGen |
| THR-149 | Plasma kallikrein inhibitor | IVit | I | Oxurion (ThromboGenics) |
| THR-317 | Anti-PIGF mAb | IVit | II | Oxurion (ThromboGenics) |
| Tocilizumab | Anti-IL-6 | IVit | II | University of Nebraska |
| Ubiquinone | Antioxidant | PO | IIa | University of Guadalajara, Mexico |
| Ziv-aflibercept | Anti-VEGF | IVit | II | Shahid Beheshti University of Medical Sciences |
Abbreviations: IV, Intravenous; IVit, Intravitreal; PO, Oral; SC, Subcutaneous; SConj, Subconjunctival; ST, Sub-tenons; Top, Topical.