verteporfin

Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.

Lemuteporfin is a light-activated photosensitizing agent that is rapidly internalized by viable cells, localizing within the cytoplasm and associating with mitochondria. This localization is a key characteristic that confers strong cytotoxic potential upon light activation. Lemuteporfin has demonstrated the ability to reduce sebaceous gland volume in preclinical animal studies. It is currently under investigation in relation to benign prostatic hyperplasia and in topical form for the management of androgenetic alopecia.

HS-291, a HtpG inhibitor targeting Borrelia burgdorferi (Bb), comprises BX-2819 (high affinity for Bb HtpG), a PEG linker, and Verteporfin (a photoactive toxin). Upon light activation, HS-291 generates reactive oxygen species that oxidize HtpG and selectively inactivate nearby proteins, leading to the rapid and irreversible inactivation of Bb [1].

MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. This compound delivers Verteporfin to CD206+ tumor-associated macrophages (TAM), thereby inhibiting the YAP/TAZ signaling pathway. It facilitates YAP exclusion from the nucleus, induces TAM polarization toward an anti-tumor phenotype, enhances phagocytosis and antigen presentation, and promotes T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.