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111In-IMP288

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

**Description:** 111In-IMP288 is a radiolabeled peptide used as a hapten in pretargeted radioimmunotherapy and imaging. It consists of the peptide IMP288 conjugated with the chelator DOTA for stable binding of radionuclides such as indium‑111 (^111In), yttrium‑90 (^90Y), or lutetium‑177 (^177Lu)[1][6][8]. The molecule contains two histamine-succinyl-glycine (HSG) moieties that allow it to bind specifically to bispecific monoclonal antibodies targeting HSG. In clinical and preclinical studies, ^111In-labeled IMP288 is administered after pretargeting tumors with an anti-HSG bispecific antibody (such as TF2 or TF10), enabling high tumor uptake and rapid clearance from non-target tissues[1][3][5]. Its primary mechanism involves acting as a radiolabeled hapten for SPECT or PET imaging and targeted radiotherapy in cancers expressing relevant antigens such as Trop‑2[2]. The compound has been investigated mainly for use in metastatic colorectal carcinoma, non-small cell lung cancer, small cell lung cancer, and other neoplasms[2].

Other names
111In-Labeled 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA)-d-Tyr-d-Lys(HSG)-d-Glu-d-Lys(HSG)-NH2 (IMP-288)IMP288IMP-288IMP 288
02

Targets

TACSTD2 (Tumor-associated calcium signal transducer 2)

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