Preferred Label : Anti-CD73 Monoclonal Antibody PT199;
NCIt definition : A humanized monoclonal antibody directed against the human ectoenzyme 5'-ecto-nucleotidase
(cluster of differentiation 73; CD73; 5'-NT; ecto-5'-nucleotidase; NT5E), with potential
immunomodulating and antineoplastic activities. Upon administration, anti-CD73 monoclonal
antibody PT199 targets and directly binds to an epitope that is in or near the CD73
catalytic domain, thereby non-competitively and fully inhibiting both soluble shed
CD73 and membrane-bound CD73 activity. This prevents CD73-mediated conversion of extracellular
adenosine monophosphate (AMP) to adenosine and the adenosine-mediated suppression
of lymphocyte activity and trafficking. This attenuates the adenosine-induced immunosuppression
in the tumor microenvironment (TME), increases the activity of cytotoxic T-lymphocytes
(CTLs), activates macrophages and reduces the activity of both myeloid-derived suppressor
cells (MDSCs) and regulatory T-lymphocytes (Tregs). By abrogating the inhibitory effect
on the immune system and enhancing the CTL-mediated immune response against cancer
cells, tumor cell growth is decreased. CD73, a plasma membrane protein belonging to
the 5'-nucleotidase (NTase) family, is upregulated on a number of cancer cell types
and catalyzes the conversion of extracellular nucleotides, such as AMP, to membrane-permeable
nucleosides, such as adenosine; it plays a key role in adenosine-mediated immunosuppression
within the TME. PT199 may inhibit the CD73 enzyme activity by preventing the transition
of CD73 from the open to the closed conformation.;
Molecule name : PT-199; PT 199;
NCI Metathesaurus CUI : CL1799081;
Origin ID : C190695;
UMLS CUI : C5783864;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target
