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177Lu-DOTA-TATE + olaparib
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
177Lu-DOTA-TATE + olaparib is an investigational combination therapy consisting of a radiopharmaceutical, 177Lu-DOTA-TATE (Lutathera), and a small molecule PARP inhibitor, olaparib (Lynparza). 177Lu-DOTA-TATE is a peptide receptor radionuclide therapy (PRRT) that targets somatostatin receptors on neuroendocrine tumor cells, delivering targeted radiation to induce DNA damage. Olaparib inhibits poly(ADP-ribose) polymerase (PARP), impairing the repair of single-strand DNA breaks. The rationale for combining these agents is to potentiate the cytotoxic effects of PRRT by preventing tumor cells from repairing radiation-induced DNA damage, thereby increasing cell death. This combination is being studied primarily in patients with somatostatin receptor-positive neuroendocrine tumors[1][2][3][4][6].
- Brand names
- LutatheraLynparza
- Other names
- Lutetium Lu 177 dotatateDOTA0-Tyr3-OctreotateDOTA-0-Tyr3-OctreotateDOTA 0-Tyr3-OctreotateAZD2281AZD-2281AZD 2281
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)SSTR5 (Somatostatin receptor 5)SSTR2 (Somatostatin receptor type 2)
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