Target intelligence / Profile preview

Costimulatory molecule

Molecular classification
Cell surface molecule, Immune checkpoint (some members), Ligand (for receptors such as CD28, CTLA-4)
01

Overview

Costimulatory molecules are a heterogeneous group of cell-surface and transmembrane proteins expressed mainly on antigen-presenting cells such as dendritic cells and B cells; they provide essential secondary signals (beyond antigen recognition) required for full T cell activation, function, and fate decisions. Key families include the B7 family (CD80/B7-1, CD86/B7-2), TNF receptor/ligand family (e.g., CD40, OX40L), among others. These molecules can deliver either activating or inhibitory signals, thereby shaping immune responses towards activation (immunity), tolerance, or regulation, and are therefore important therapeutic targets in cancer, transplantation, and autoimmune diseases. However, “costimulatory molecules” is a collective term; further specification is required to reference an individual drug target molecule.

Other names
Costimulation moleculesCo-stimulatory moleculesSignal II molecules
02

Mechanism of action

Immune checkpoint inhibition or blockade (e.g., blocking CTLA-4 or PD-1/PD-L1 pathways); Costimulatory blockade (e.g., abatacept prevents costimulation of T cells by binding CD80/CD86); Modulation of T cell activation—either enhancing or suppressing immune responses

03

Biological functions

Immune response modulationT cell activationRegulation of T cell differentiationInduction of tolerance or immunity
04

Disease associations

Cancer (especially as immunotherapy targets)AutoimmunityTransplant rejection and toleranceInfectionInflammation
05

Safety considerations

Risk of excessive immune activation or autoimmunity when costimulation is enhanced (as with some checkpoint inhibitors)Increased susceptibility to infections or impaired immune surveillance when costimulation is suppressed (as in therapeutic blockade—e.g., increased infection risk with abatacept)Cytokine release syndrome or systemic inflammation (for some agents or contexts)
06

Interacting drugs

Abatacept

3 more in the full profile.

07

Biomarkers

Expression levels of CD80, CD86, CD40, and others can be used as biomarkers of immune cell activation or maturity in certain diagnostic or monitoring settings

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