Population pharmacokinetics and exposure-response analyses of polatuzumab vedotin in patients with previously untreated DLBCL from the POLARIX study

CPT Pharmacometrics Syst Pharmacol. 2024 Jun;13(6):1055-1066. doi: 10.1002/psp4.13141. Epub 2024 Apr 15.

Abstract

Polatuzumab vedotin is a CD79b-directed antibody-drug conjugate that targets B cells and delivers the cytotoxic payload monomethyl auristatin E (MMAE). The phase III POLARIX study (NCT03274492) evaluated polatuzumab vedotin in combination with rituximab, cyclophosphamide, doxorubicin, and prednisone (R-CHP) as first-line treatment of diffuse large B-cell lymphoma (DLBCL). To examine dosing decisions for this regimen, population pharmacokinetic (popPK) analysis, using a previously developed popPK model, and exposure-response (ER) analysis, were performed. The popPK analysis showed no clinically meaningful relationship between cycle 6 (C6) antibody-conjugated (acMMAE)/unconjugated MMAE area under the concentration-time curve (AUC) or maximum concentration, and weight, sex, ethnicity, region, mild or moderate renal impairment, mild hepatic impairment, or other patient and disease characteristics. In the ER analysis, C6 acMMAE AUC was significantly associated with longer progression-free and event-free survival (both p = 0.01). An increase of <50% in acMMAE/unconjugated MMAE exposure did not lead to a clinically meaningful increase in adverse events of special interest. ER data and the benefit-risk profile support the use of polatuzumab vedotin 1.8 mg/kg once every 3 weeks with R-CHP for six cycles in patients with previously untreated DLBCL.

Publication types

  • Clinical Trial, Phase III
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols* / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols* / pharmacokinetics
  • Antineoplastic Combined Chemotherapy Protocols* / therapeutic use
  • Area Under Curve
  • Cyclophosphamide* / administration & dosage
  • Cyclophosphamide* / pharmacokinetics
  • Cyclophosphamide* / therapeutic use
  • Dose-Response Relationship, Drug
  • Doxorubicin* / administration & dosage
  • Doxorubicin* / analogs & derivatives
  • Doxorubicin* / pharmacokinetics
  • Doxorubicin* / therapeutic use
  • Female
  • Humans
  • Immunoconjugates / administration & dosage
  • Immunoconjugates / adverse effects
  • Immunoconjugates / pharmacokinetics
  • Lymphoma, Large B-Cell, Diffuse* / drug therapy
  • Male
  • Middle Aged
  • Models, Biological
  • Prednisone* / administration & dosage
  • Prednisone* / pharmacokinetics
  • Prednisone* / therapeutic use
  • Progression-Free Survival
  • Rituximab* / administration & dosage
  • Rituximab* / pharmacokinetics
  • Rituximab* / therapeutic use

Substances

  • polatuzumab vedotin
  • Doxorubicin
  • Cyclophosphamide
  • Prednisone
  • Rituximab
  • Immunoconjugates
  • Antibodies, Monoclonal