Molecular Partners- DARPins Technology

Abicipar

Abicipar is a DARPin-based anti-angiogenic drug for wet age-related macular degeneration (wet AMD) and diabetic macular edema (DME). Wet AMD is a leading cause of blindness in the developed world and DME is a leading cause of blindness in young adults in developed countries.

Abicipar is an antagonist of Vascular Endothelial Growth Factor A (VEGF-A) that inhibits all relevant subtypes of VEGF-A with very high potency. The combination of small size, high potency and long intra-vitreal half-life offers the potential for less frequent injections (compared to Lucentis, the current standard of care) and higher gains in visual acuity.

In Phase 2b studies, abicipar was shown to provide at least equal or higher vision gains with the potential for fewer injections in wet AMD compared to standard of care treatment Lucentis® (ranibizumab).

Phase 2b data suggests that abicipar could be administered every 12 weeks following loading doses, compared to every 4 weeks for Lucentis. Abicipar is expected to enter Phase 3 clinical trials for wet AMD in Q2 2015, in partnership with Allergan.

In Phase 1/2 clinical trials in DME, abicipar has demonstrated potential to suppress VEGF-A concentrations in aqueous humor after a single intraocular injection, with a pharmacokinetic half-life of about 2 weeks. These effects were accompanied by a stabilization or improvement in visual acuity and reduction of retinal edema (measured with optical coherence tomography) for up to 12 to 16 weeks.

We have developed abicipar in collaboration with Allergan, Inc., one of the leading global specialty biopharmaceutical companies.

Abicipar – REACH Stage 3 Study Results

Abicipar data presented at ASRS
Abicipar Chart

Click to Enlarge

Source: Allergan, 12 August 2014
Note: Not statistically significant

Multi-VEGF/PDGF DARPin

In addition to abicipar, together with Allergan we are developing further DARPins for other ocular targets. The multi-VEGF/PDGF DARPin takes an abicipar-like DARPin and adds an anti-PDGF DARPin. This pairing creates a multi-benefit therapy that targets the two critical pathways implicated in serious retinal disease.

The multi-VEGF/PDGF DARPin destabilizes the pericytes that protect new blood vessels that form in the eye during wet AMD. By stripping away the pericytes with the anti-PDGF DARPin, the blood vessels are susceptible to anti-VEGF DARPins, causing regression of the new-grown vessels.

This multi-benefit DARPin combines treatment for both anti-PDGF and anti-VEGF in a single molecule, as opposed to the current standard of care, Lucentis, which is solely an anti-VEGF treatment.

Currently, our multi -VEGF/PDGF DARPin is in preclinical studies in partnership with Allergan. This product candidate has the potential to be the first single therapy targeting both VEGF and PDGF pathways to provide improved visual outcomes for all wet AMD patients.