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Di-HSG DOTA peptide (IMP-288) (IMP-288)

Target
IMP-288
Molecular classification
Other: Synthetic peptide hapten
01

Overview

IMP-288 is a synthetic di-HSG peptide, engineered to serve as a radiolabeled hapten for pretargeted radioimmunotherapy and imaging in oncology. It contains moieties (histamine-succinyl-glycine, HSG) that bind with high affinity to specific bispecific antibodies pretargeted to tumor antigens such as carcinoembryonic antigen (CEA) or trophoblast cell surface antigen 2 (Trop-2). The DOTA chelator allows labeling with a variety of radioisotopes (e.g., 177Lu, 111In, 68Ga), enabling applications in PET/SPECT imaging and targeted radiation therapy. IMP-288 itself is not a receptor, enzyme, or transporter, and has no endogenous biological activity. It enables highly specific targeting of radiotherapy to tumors, with rapid renal clearance of unbound peptide reducing off-target systemic toxicity. Clinical investigations have explored its safety and efficacy in several solid tumor indications, predominantly colorectal cancer, pancreatic cancer, and prostate cancer.

Other names
Di-HSG DOTA peptideIMP288DOTA-di-HSG peptide[111In]IMP-288[177Lu]IMP-288[68Ga]IMP-288Hapten-peptide IMP288
02

Mechanism of action

Pretargeted delivery: After administration of a bispecific antibody specific for both a tumor antigen (e.g., CEA or Trop-2) and the HSG hapten, IMP-288 is injected and selectively binds to the tumor-localized antibody, delivering a radioactive payload for imaging (PET/SPECT) or therapy (PRIT). Rapid clearance/reduced toxicity: Unbound IMP-288 is rapidly eliminated through the kidneys due to its small size, reducing systemic radioactivity exposure.

03

Biological functions

Facilitator for targeted imaging and therapy when paired with bispecific antibodies in pretargeted radioimmunotherapy (PRIT) or immuno-PETCarrier for therapeutic radioisotopes (e.g., 177Lu, 111In, 68Ga)Not involved in endogenous cellular signaling, metabolism, or other biological functions
04

Disease associations

Cancer (colorectal cancer, non-small cell lung cancer, pancreatic cancer, and other solid tumors)Used as a diagnostic and therapeutic tool, not as a direct marker or effector
05

Safety considerations

Renal toxicity: Rapid elimination through kidneys, with potential for renal uptake when labeled with certain radioisotopes (e.g., 213Bi, 177Lu)Histamine reaction: Use of anti-histamines is sometimes needed, as IMP-288 can include HSG moietiesTherapeutic index: Optimized by rapid clearing and selective tumor targeting; off-target toxicity generally low
06

Interacting drugs

Bispecific antibodies: especially TF2 (anti-CEA/anti-HSG)

2 more in the full profile.

07

Biomarkers

None specific for IMP-288 itself.Indirectly used: Expression of target tumor antigens (e.g., CEA, Trop-2) for which the bispecific antibody component is specific

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