Polatuzumab vedotin

Polatuzumab vedotin
Monoclonal antibody
Type ?
Source Humanized (from mouse)
Target CD79b
Clinical data
Synonyms DCDS4501A, RG7596
ATC code
  • none
Identifiers
CAS Number
IUPHAR/BPS
ChemSpider
  • none
KEGG
Chemical and physical data
Formula C6670H10317N1745O2087S40
Molar mass 149.6 kg/mol

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 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.

Clinical 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

  1. ↑ World Health Organization (2012). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 108" (PDF). WHO Drug Information. 26 (4).
  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)


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