Developability Assessment of Physicochemical Properties and Stability Profiles of HIV-1 BG505 SOSIP.664 and BG505 SOSIP.v4.1-GT1.1 gp140 Envelope Glycoprotein Trimers as Candidate Vaccine Antigens

J Pharm Sci. 2019 Jul;108(7):2264-2277. doi: 10.1016/j.xphs.2019.01.033. Epub 2019 Feb 15.

Abstract

The induction of broadly neutralizing antibodies (bNAbs) is a major goal in the development of an effective vaccine against HIV-1. A soluble, trimeric, germline (gI) bNAb-targeting variant of the HIV-1 envelope glycoprotein (termed BG505 SOSIP.v4.1-GT1.1 gp140, abbreviated to GT1.1) has recently been developed. Here, we have compared this new immunogen with the parental trimer from which it was derived, BG505 SOSIP.664 gp140. We used a comprehensive suite of biochemical and biophysical methods to determine physicochemical similarities and differences between the 2 trimers, and thereby assessed whether additional formulation development efforts were needed for the GT1.1 vaccine candidate. The overall higher order structure and oligomeric states of the 2 vaccine antigens were quite similar, as were their thermal, chemical, and colloidal stability profiles, as evaluated during accelerated stability studies. Overall, we conclude that the primary sequence changes made to create the gl bNAb-targeting GT1.1 trimer did not detrimentally affect its physicochemical properties or stability profiles from a pharmaceutical perspective. This developability assessment of the BG505 GT1.1 vaccine antigen supports using the formulation and storage conditions previously identified for the parental SOSIP.664 trimer and enables the development of GT1.1 for phase I clinical studies.

Keywords: BG505; HIV-1 Env; developability assessment; formulation; gp140; stability; trimers; vaccine.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Neutralizing / immunology
  • Antigens, Viral / immunology*
  • Epitopes / immunology
  • Glycoproteins / immunology*
  • HIV Antibodies / immunology*
  • HIV-1 / immunology*
  • Humans
  • Protein Multimerization / immunology
  • env Gene Products, Human Immunodeficiency Virus / immunology*

Substances

  • Antibodies, Neutralizing
  • Antigens, Viral
  • Epitopes
  • GP 140
  • Glycoproteins
  • HIV Antibodies
  • env Gene Products, Human Immunodeficiency Virus