Druggability & Clinical Context
Druggability
Low
Score: 0.45
Druggability Analysis
Structural Tractability0.70
Key Metrics
PDB Structures:
5
Known Drugs:
1
Approved:
1
In Clinical Trials:
0
Drug Pipeline (1 compounds)
1 Approved
Druggability Rationale: ANGPT1 is highly druggable (0.80 score) due to its well-characterized protein structure with 5 available PDB structures at high resolution (1.75 Γ
), established precedent with approved therapeutic Faricimab, and validated Tie2 signaling pathway. The secreted protein nature and ligand-based mechanism make it amenable to both protein therapeutics and small molecule mimetic approaches.
Mechanism: Protein therapeutics or small molecule mimetics activating Tie2 signaling
Drug Pipeline (1 compounds)
1 Approved
Known Drugs:Faricimab (approved) β Neovascular age-related macular degeneration
Structural Data:PDB (5) βAlphaFold βCryo-EM β
Selectivity & Safety Considerations
ANGPT1 selectivity is advantageous as it specifically targets the Tie2 receptor pathway with minimal known off-targets; however, care must be taken to avoid cross-reactivity with ANGPT2 or other angiopoietin family members. The main selectivity challenge involves achieving Tie2-specific activation while avoiding unintended vascular permeability changes in non-target tissues.
Clinical Trials (7)
Relevant trials from ClinicalTrials.gov
By Phase
NA: 1 Β· PHASE2: 2 Β· PHASE4: 2 Β· Unknown: 2
PHASE4
NCT06709339
n=120
Polypoidal Choroidal Vasculopathy
Interventions: Faricimab Injection [Vabysmo]
Sponsor: Association for Innovation and Biomedical Research on Light | Started: 2025-08-06
PHASE4
NCT06875245
n=100
Wet Age-related Macular Degeneration
Interventions: Faricimab Injection
Sponsor: Faculty Hospital Kralovske Vinohrady | Started: 2023-03-31
PHASE2
NCT04597918
n=99
Diabetic Macular Edema
Interventions: Faricimab
Sponsor: Hoffmann-La Roche | Started: 2020-11-25
PHASE2
NCT07093385
n=43
Age-Related Macular Degeneration
Interventions: Faricimab Injection
Sponsor: University of Baghdad | Started: 2024-09-10
NA
NCT07144865
n=8
Proliferative Diabetic Retinopathy
Interventions: conbercept ophthalmic injection οΌ0.5mgοΌ, Faricimab
Sponsor: Bojie Hu | Started: 2024-12-01
Unknown
NCT06124677
n=46
Neovascular Age-related Macular Degenera
Interventions: Faricimab
Sponsor: Rigshospitalet, Denmark | Started: 2023-11-01
Unknown
NCT06231121
n=13
Neovascular Age-related Macular Degenera
Interventions: Faricimab
Sponsor: Rigshospitalet, Denmark | Started: 2023-12-01