| 词条 | Polatuzumab vedotin |
| 释义 |
| type = mab | image = | alt = | mab_type = | source = zu/o | target = CD79b | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 1313206-42-6 | ATC_prefix = none | ATC_suffix = | PubChem = | IUPHAR_ligand = 8404 | DrugBank = | ChemSpiderID = none | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D10761 | C=6670 | H=10317 | N=1745 | O=2087 | S=40 | molecular_weight = 149.6 kg/mol | synonyms = DCDS4501A, RG7596 }}Polatuzumab vedotin (INN[1]) (DCDS4501A or RG7596) is an antibody-drug conjugate or ADC designed for the treatment of cancer.[2] The investigational drug, being developed by Genentech/Roche, contains a humanized monoclonal antibody (mAb) targeting CD79b (B-cell antigen receptor complex-associated protein beta chain) conjugated to the synthetic dolastatin 10 analog microtubule-disrupting monomethyl auristatin E (MMAE) through engineered cysteines (THIOMABs) via a protease-cleavable peptide linker (valine–citrulline; Maleimidocaproylvaline-citrulline-p-aminobenzoyloxycarbonyl or MC-VC-PABC). The advantage of the citrulline-valine (VC) linker being used that it is highly stable in plasma.[3] Mechanism of ActionUpon administration, polatuzumab vedotin selectively binds to CD79b, a protein which is abundantly expressed on the surface of B-cells. Following internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. Clinical trialsPolatuzumab vedotin is being investigated in Phase I and Phase II clinical trials. The Phase I trial investigates the drug in B-cell non-Hodgkin’s lymphoma [4] while the Phase II trials investigates the trial drug for the treatment of patients with relapsed or refractory follicular or diffuse large B-Cell Lymphoma.[5] References1. ^{{cite journal | author = World Health Organization | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 108 | journal = WHO Drug Information | volume = 26 | issue = 4 | year = 2012 | url = http://www.who.int/medicines/publications/druginformation/innlists/PL108.pdf | format=PDF}} {{monoclonals for tumors}}{{monoclonal-antibody-stub}}2. ^Statement On A Nonproprietary Name Adopted By The USAN Council - Polatuzumab Vedotin, American Medical Association - Needs login/subscription. 3. ^Polatuzumab vedotin (Drug Description) 4. ^NCT01992653 (Clinical Trial / Polatuzumab Vedotin / DCDS4501A / RG-7596) 5. ^NCT02257567 (Clinical Trial / Polatuzumab Vedotin / DCDS4501A / RG-7596) 1 : Monoclonal antibodies |
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