Preferred Label : FAP/CD40-targeting DARPin MP0317;
NCIt synonyms : FAP/CD40-targeting Designed Ankyrin Repeat Protein MP0317; Anti-CD40/Anti-FAP DARPin Agent MP0317; FAP x CD40-targeting DARPin MP0317;
NCIt definition : A tri-specific, designed ankyrin repeat proteins (DARPin)-based agent targeting the
tumor-associated protein fibroblast activation protein (FAP), CD40 receptor and human
serum albumin (HSA), with potential immunostimulatory and antineoplastic activities.
Upon administration, FAP/CD40-targeting DARPin MP0317 targets and binds to both FAP,
localized predominantly on cancer-associated fibroblasts (CAFs) in the tumor stroma,
and CD40, a cell surface stimulatory receptor expressed on various immune cells including
B-lymphocytes, monocytes and dendritic cells (DCs). The simultaneous binding to FAP
and CD40 results in local clustering of FAP-expressing tumor stromal cells and CD40-expressing
immune cells. Activation of CD40 induces proliferation and activation of B-lymphocytes,
shifts the induction of suppressive macrophages towards immunostimulatory macrophages,
activates monocyte-derived DCs (moDCs), and leads to the secretion of inflammatory
cytokines, which activates the immune system to induce the proliferation and activation
of cytotoxic T-lymphocytes (CTLs) against tumor cells. CD40, a member of the tumor
necrosis factor receptor superfamily (TNFRSF), plays a key role in the activation
of the immune system. FAP is abundantly expressed by CAFs in the majority of solid
tumors. HSA binding prolongs the half-life of MP0317. Compared to antibodies, DARPins
are small in size, have favorable pharmacokinetics and allow for both high affinity
binding and efficacy.;
Molecule name : MP 0317; MP-0317;
NCI Metathesaurus CUI : CL1773495;
Origin ID : C185164;
UMLS CUI : C5666958;
Semantic type(s)
- concept_is_in_subset
- has_target
