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niraparib + tebotelimab
- Development stage
- Discontinued
- Lead developer
- MacroGenics
- Modality
- Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Niraparib + tebotelimab is an investigational combination therapy consisting of niraparib, an oral poly(ADP-ribose) polymerase (PARP) inhibitor, and tebotelimab (MGD013), a first-in-class bispecific monoclonal antibody targeting PD-1 and LAG-3. Developed by Zai Lab in collaboration with MacroGenics, this combination aims to leverage the synergistic effects of PARP inhibition and dual immune checkpoint blockade. Niraparib induces DNA damage and promotes an inflammatory tumor microenvironment, while tebotelimab reactivates exhausted T cells by simultaneously blocking the PD-1 and LAG-3 pathways. The combination was evaluated in Phase 1b trials for advanced solid tumors, including gastric cancer, triple-negative breast cancer, biliary tract carcinoma, and endometrial carcinoma. However, due to limited antitumor activity, further clinical development for this specific combination has been discontinued.
- Other names
- niraparib + tebotelimabtebotelimab + niraparib
02
Targets
LAG3 (Lymphocyte activation Gene-3 protein)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)PDCD1 (Programmed cell death protein 1 receptor)Pol II (RNA polymerase II elongation factors)
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