Polatuzumab vedotin

Polatuzumab vedotin
Monoclonal antibody
Type	?
Source	Humanized (from mouse)
Target	CD79b
Clinical data
ATC code	none
Identifiers
CAS Number	1313206-42-6
IUPHAR/BPS	8404
ChemSpider	none
Chemical and physical data
Formula	C₆₆₇₀H₁₀₃₁₇N₁₇₄₅O₂₀₈₇S₄₀
Molar mass	149.6 kg/mol

Polatuzumab vedotin^[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 Action

Upon 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.

Clincal trials

Polatuzumab 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]

References

↑ World Health Organization (2012). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 108" (PDF). WHO Drug Information. 26 (4).
↑ Statement On A Nonproprietary Name Adopted By The USAN Council - Polatuzumab Vedotin, American Medical Association - Needs login/subscription.
↑ Polatuzumab vedotin (Drug Description)
↑ NCT01992653 (Clinical Trial / Polatuzumab Vedotin / DCDS4501A / RG-7596)
↑ NCT02257567 (Clinical Trial / Polatuzumab Vedotin / DCDS4501A / RG-7596)

Monoclonal antibodies for tumors

Tumor
("-t(u[m])-")

Human ("-tumu-")	Adecatumumab Cixutumumab Conatumumab Daratumumab Drozitumab Duligotumab Dusigitumab Enfortumab vedotin Figitumumab Ganitumab Glembatumumab vedotin Intetumumab Iratumumab Lexatumumab Lucatumumab Mapatumumab Narnatumab Necitumumab Ofatumumab Olaratumab Panitumumab Patritumab Pritumumab Radretumab Rilotumumab Robatumumab Seribantumab Tarextumab Teprotumumab Tovetumab Vantictumab Votumumab Zalutumumab "-melu-" (melanoma) Flanvotumab

Mouse ("-tumo-")	Altumomab pentetate Anatumomab mafenatox Arcitumomab Bectumomab Blinatumomab Detumomab Ibritumomab tiuxetan Minretumomab Mitumomab Moxetumomab pasudotox Naptumomab estafenatox Nofetumomab merpentan Pemtumomab^† Pintumomab Racotumomab Satumomab pendetide Solitomab Taplitumomab paptox Tenatumomab Tositumomab 3F8 "-govo-" (ovarian tumor) Abagovomab Igovomab Oregovomab "-pro-" (prostate tumor) Capromab pendetide "-colo-" (colonic tumor) Edrecolomab Nacolomab tafenatox

Chimeric ("-tuxi-")	Amatuximab Bavituximab Brentuximab vedotin Cetuximab Derlotuximab biotin Dinutuximab Ensituximab Futuximab Girentuximab Indatuximab ravtansine Isatuximab Margetuximab Rituximab Siltuximab Ublituximab "-mexi-" (melanoma): Ecromeximab

Humanized ("-tuzu-")	Abituzumab Alemtuzumab Bevacizumab Bivatuzumab mertansine Brontictuzumab Cantuzumab mertansine Cantuzumab ravtansine Citatuzumab bogatox Clivatuzumab tetraxetan Dacetuzumab Dalotuzumab Denintuzumab mafodotin Elotuzumab Emactuzumab Emibetuzumab Enoblituzumab Etaracizumab Farletuzumab Ficlatuzumab Gemtuzumab ozogamicin Imgatuzumab Inotuzumab ozogamicin Labetuzumab Lifastuzumab vedotin Lintuzumab Lorvotuzumab mertansine Lumretuzumab Matuzumab^§ Milatuzumab Nimotuzumab Obinutuzumab Ocaratuzumab Otlertuzumab Onartuzumab Oportuzumab monatox Parsatuzumab Pertuzumab Pinatuzumab vedotin Polatuzumab vedotin Sibrotuzumab Simtuzumab Tacatuzumab tetraxetan Tigatuzumab Trastuzumab Tucotuzumab celmoleukin Vandortuzumab vedotin Veltuzumab Vorsetuzumab mafodotin "-gozu-" (ovarian tumor) Sofituzumab vedotin

Rat/mouse hybrid ("-tumaxo-")	Catumaxomab Ertumaxomab

Chimeric + humanized ("-tuxizu-")	Depatuxizumab mafodotin Ontuxizumab

Veterinary ("-tuvet-")	Blontuvetmab Tamtuvetmab

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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