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CTP-AP39
- Development stage
- Preclinical
- Lead developer
- Beijing An Zhen Hospital
- Modality
- Small Molecules, Peptides, Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
CTP-AP39 (also known as CTP-AP39-DSPE-PEG) is a preclinical-stage, cardiac-targeted, mitochondria-directed hydrogen sulfide (H2S) delivery system [ehag785.4592]. It consists of the mitochondria-targeted H2S donor AP39 encapsulated within a DSPE-PEG-based lipid nanocarrier, with the surface decorated with a cardiac-targeting peptide (CTP) to enable selective accumulation in myocardial tissue [ehag785.4592]. AP39 itself is a slow-release H2S donor containing a triphenylphosphonium (TPP) targeting motif linked to an H2S-donating dithiolethione moiety, allowing it to accumulate selectively in the mitochondria. CTP-AP39 is being investigated for the treatment of diabetic cardiomyopathy (DCM), where it has been shown to restore myocardial bioenergetics, improve left ventricular systolic and diastolic function, and attenuate cardiac remodeling, hypertrophy, and fibrosis by modulating signaling at the endoplasmic reticulum-mitochondria interface (specifically the ITPR3-GRP75-VDAC1 axis) [ehag785.4592].
- Other names
- CTP-AP39-DSPE-PEGCTP-AP-39-DSPE-PEGCTP-AP 39-DSPE-PEGCTP–AP39–DSPE-PEG
02
Targets
EAG2-Kvβ2 (EAG2–Kvβ2 complex)
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