Induction of tolerance to factor VIII by transient co-administration with rapamycin

J Thromb Haemost. 2011 Aug;9(8):1524-33. doi: 10.1111/j.1538-7836.2011.04351.x.

Abstract

Background: Formation of inhibitory antibodies is a frequent and serious complication of factor (F) VIII replacement therapy for the X-linked bleeding disorder hemophilia A. Similarly, hemophilia A mice develop high-titer inhibitors to recombinant human FVIII after a few intravenous injections.

Objective: Using the murine model, the study sought to develop a short regimen capable of inducing tolerance to FVIII.

Methods: A 1-month immunomodulatory protocol, consisting of FVIII administration combined with oral delivery of rapamycin, was developed.

Results: The protocol effectively prevented formation of inhibitors to FVIII upon subsequent intravenous treatment (weekly for 3.5 months). Control mice formed high-titer inhibitors and had CD4(+) T effector cell responses characterized by expression of IL-2, IL-4 and IL-6. Tolerized mice instead had a CD4(+)CD25(+)FoxP3(+) T cell response to FVIII that suppressed antibody formation upon adoptive transfer, indicating a shift from Th2 to Treg if FVIII antigen was introduced to T cells during inhibition with rapamycin. CD4(+) T cells from tolerized mice also expressed TGF-β1 and CTLA4, but not IL-10. The presence of FVIII antigen during the time of rapamycin administration was required for specific tolerance induction.

Conclusions: The study shows that a prophylactic immune tolerance protocol for FVIII can be developed using rapamycin, a drug that is already widely in clinical application. Immune suppression with rapamycin was mild and highly transient, as the mice regained immune competence within a few weeks.

Publication types

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

MeSH terms

  • Adoptive Transfer
  • Animals
  • Antibodies / blood*
  • CD4-Positive T-Lymphocytes / drug effects*
  • CD4-Positive T-Lymphocytes / immunology
  • CD4-Positive T-Lymphocytes / transplantation
  • CTLA-4 Antigen / metabolism
  • Cells, Cultured
  • Coagulants / administration & dosage*
  • Coagulants / immunology
  • Disease Models, Animal
  • Drug Administration Schedule
  • Factor VIII / administration & dosage*
  • Factor VIII / immunology
  • Forkhead Transcription Factors / metabolism
  • Hemophilia A / blood
  • Hemophilia A / drug therapy*
  • Hemophilia A / immunology
  • Humans
  • Immune Tolerance / drug effects*
  • Immunosuppressive Agents / administration & dosage*
  • Interleukin-2 / metabolism
  • Interleukin-2 Receptor alpha Subunit / metabolism
  • Interleukin-4 / metabolism
  • Interleukin-6 / metabolism
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Recombinant Proteins / administration & dosage
  • Sirolimus / administration & dosage*
  • Time Factors
  • Transforming Growth Factor beta1 / metabolism

Substances

  • Antibodies
  • CTLA-4 Antigen
  • Coagulants
  • Ctla4 protein, mouse
  • Forkhead Transcription Factors
  • Foxp3 protein, mouse
  • Il2ra protein, mouse
  • Immunosuppressive Agents
  • Interleukin-2
  • Interleukin-2 Receptor alpha Subunit
  • Interleukin-6
  • Recombinant Proteins
  • Tgfb1 protein, mouse
  • Transforming Growth Factor beta1
  • Interleukin-4
  • F8 protein, human
  • Factor VIII
  • Sirolimus