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| | Lambrolizumab Basic information |
| Product Name: | Lambrolizumab | | Synonyms: | Lambrolizumab;Pembrolizumab;pembrolimumab;Pembrolizumab (anti-PD-1);PEMBROLIMUMAB PD-1 1374853-91-4;Pembrolizumab 25mg/ml;PembrolizumabQ: What is
Pembrolizumab Q: What is the CAS Number of
Pembrolizumab Q: What is the storage condition of
Pembrolizumab Q: What are the applications of
Pembrolizumab;Research Grade Pembrolizumab(DHH02202) | | CAS: | 1374853-91-4 | | MF: | | | MW: | 0 | | EINECS: | 807-012-2 | | Product Categories: | | | Mol File: | Mol File | ![Lambrolizumab Structure]() |
| | Lambrolizumab Chemical Properties |
| storage temp. | Store at -80°C | | CAS DataBase Reference | 1374853-91-4 |
| | Lambrolizumab Usage And Synthesis |
| Uses | A recombinant, single-chain, anti-CD19/anti-CD3 bispecific monoclonal antibody with potential immunostimulating and antineoplastic activities. | | Clinical Use | Humanised monoclonal antibody:
Treatment of advanced melanoma
Treatment of non-small cell lung carcinoma (NSLC)
Treatment of relapsed or refractory classical
Hodgkin lymphoma (cHL)
Treatment of urothelial carcinoma | | Enzyme inhibitor | This humanized receptor-directed monoclonal antibody and anticancer agent (MW = 146.3 kDa; CAS 1374853-91-4), also known by its code name MK-3475, its former name lambrolizumab, and its trade name Keytruda?, targets the Programmed Death-1 (PD-1 or Pdcd1) receptor, a well-known negative regulator of T-cell effector mechanisms that limits immune responses against cancer. Having received "Breakthrough Therapy" designation in April, 2013 to expedite its development as a melanoma therapy, pembrolizumab won final FDA approval in September, 2014. Mechanism of Inhibitor Action: An immunoreceptor belonging to the CD28/CTLA-4 family, PD-1 negatively regulates antigen receptor signaling by recruiting the protein tyrosine phosphatase SHP-2, after interacting with either of two ligands, PD-L1 or PD-L2. With its wide range of ligand distribution in the body, PD-1 is significant in nearly every aspect of immune responses (e.g. autoimmunity, tumor immunity, infectious immunity, transplantation immunity, allergy and immunological privilege). Pembrolizumab blocks the interaction between PD-1 and its ligands, PD-L1 and PD-L2. PD-1 and related target PD-ligand 1 (PD-L1) are normally expressed on the surface of activated T cells, and formation of the PDL1·PD-1 complex inhibits immune activation and reduces T-cell cytotoxic activity when bound. This negative feedback loop maintains normal immune responses by limiting T-cell activity and thereby protecting normal cells during chronic inflammation. Tumor cells can circumvent T-cell– mediated cytotoxicity by expressing PD-L1 on their outer surface or on tumor-infiltrating immune cells to inhibit immune-mediated tumor cell killing. Use of pembrolizumab is indicated in the treatment of patients with unresectable or metastatic melanoma and disease progression following ipilimumab, especially if positive for the BRAFV600 mutation. MK3475 is also highly selective, humanized monoclonal IgG4-k isotype antibody against PD-1 that is designed to block the negative immune regulatory signaling of the PD-1 receptor on T cells. Inhibitor Design: To preparepembrolizumab, the variable region sequences of a very high affinity (Kd = 28 pM) mouse anti-human PD-1 antibody were grafted into a human IgG4 immunoglobulin with a stabilizing Ser-228-Pro alteration in Fc receptors. The IgG4 subtype does not engage Fc receptors and does not activate complement, thereby avoiding cytotoxic effects of the antibody when it binds to the T cells that it is intended to activate. Pharmacokinetics: The recommended dose (2 mg/kg) is administered as an intravenous infusion over 30 minutes every 3 weeks, or until disease progression resumes or toxicity becomes unacceptable. Its steady-state concentration is reached by 18 weeks. (Half-life: 26 days; Clearance: 0.22 L/day) | | Drug interactions | Potentially hazardous interactions with other drugs
Vaccines: risk of generalised infections with live
vaccines - avoid. | | Metabolism | Pembrolizumab undergoes catabolism to small peptides
and single amino acids via general protein degradation
routes and does not rely on metabolism for clearance. |
| | Lambrolizumab Preparation Products And Raw materials |
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