Keytruda 3D Moving Molecular Structure PDB: 5DK3
Pembrolizumab Fab bound to human PD-1 receptor (2.28 Å resolution)
Keytruda 3D Mechanism of Action (MOA) PD-1 Checkpoint
Reactivating cytotoxic T-lymphocytes by blocking PD-1 / PD-L1 immune brake
1. Normal Immune Response & T-Cell Activation
MHC-TCR recognition activates cytotoxic T-cells
Tumor cells overexpress PD-L1. When PD-L1 engages PD-1 on CD8+ T-cells, it initiates inhibitory SHP-2 phosphatase signaling, turning off T-cell proliferation and cytolytic activity.
Drug Master Record: Pembrolizumab
Active Global BlockbusterINN: Pembrolizumab (rDNA origin) | Proprietary Name: KEYTRUDA® | Manufacturer: Merck Sharp & Dohme (MSD)
Sept 4, 2014 (Advanced Melanoma)
Humanized IgG4-kappa monoclonal antibody that binds PD-1 with high affinity (KD ~ 29 pM), preventing engagement with PD-L1 and PD-L2 to release anti-tumor immune suppression.
Target: PD-1 (CD279)
Mass: ~149 kDa
Structure: PDB 5DK3 (2.28 Å)
ATC Code: L01FF02
Vial: 100 mg/4 mL solution.
Dilution: 0.9% NaCl or 5% Dextrose.
Storage: 2°C to 8°C. Do not freeze or shake.
Adults: 200 mg Q3W or 400 mg Q6W IV over 30 min.
Pediatrics: 2 mg/kg (max 200 mg) Q3W.
Duration: Up to 24 months or progression.
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