Druggability & Clinical Context
Druggability
Medium
Score: 0.55
Druggability Analysis
Structural Tractability0.70
Key Metrics
PDB Structures:
4
Known Drugs:
2
Approved:
1
In Clinical Trials:
0
Drug Pipeline (2 compounds)
1 Approved ยท 1 Preclinical
Druggability Rationale: SLC7A11 demonstrates medium druggability (0.55) supported by existing approved drug (sulfasalazine) and robust structural data (4 PDB structures, cryo-EM, AlphaFold), confirming ligand-binding capability. However, transporter inhibition requires achieving selective blockade of cystine/glutamate exchange without disrupting other critical SLC7A-family functions, and achieving blood-brain barrier penetration remains challenging for neurodegenerative applications.
Mechanism: Small molecule inhibition of cystine/glutamate exchange
Drug Pipeline (2 compounds)
1 Approved ยท 1 Preclinical
Known Drugs:Sulfasalazine (approved) โ inflammatory bowel disease
Erastin (preclinical) โ cancer research
Structural Data:PDB (4) โAlphaFold โCryo-EM โ
Selectivity & Safety Considerations
SLC7A11 selectivity is achievable given its unique heterodimerization requirement with 4F2hc; however, off-target effects on related SLC7A family members (SLC7A1, SLC7A2) must be evaluated. Species differences in transporter pharmacology and potential compensatory transporter activation present additional selectivity concerns in chronic dosing.
Clinical Trials (4)
Relevant trials from ClinicalTrials.gov
By Phase
NA: 1 ยท PHASE3: 3
PHASE3
NCT06060301
n=46
Oral Lichen Planus, Topical Sulfasalazine, Corticosteroids
Interventions: sulfasalazine 500 MG, corticosteroids
Sponsor: Cairo University | Started: 2023-03-01
PHASE3
NCT02057250
n=217
RA
Interventions: Sarilumab, Auto-Injector Device (AID), Pre-filled Syringe (PFS)
Sponsor: Sanofi | Started: 2014-03
PHASE3
NCT06985134
n=93
Comparative Efficacy and Safety of Thali, Condition ...Moderate to Severe Axial Sp
Interventions: Comparative Efficacy and Safety of Thali
Sponsor: Bangabandhu Sheikh Mujib Medical University, Dhaka, Banglade | Started: 2017-01-01
NA
NCT00405275
n=353
Rheumatoid Arthritis
Interventions: Etanercept, methotrexate, Sulfasalazine
Sponsor: US Department of Veterans Affairs | Started: 2007-07