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New targeted chemotherapies using small-molecule-drug conjugates (SMDC) show promise for treating metastatic prostate cancer. A novel pH-responsive linker improved efficacy and survival in mice, delivering potent drugs specifically to tumors with minimal toxicity.

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Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Metastatic prostate cancer necessitates novel therapeutics to overcome high mortality and off-target toxicity.
  • Prostate-specific membrane antigen (PSMA) is a validated target for prostate cancer therapy.
  • Small-molecule-drug conjugates (SMDC) offer a strategy for targeted drug delivery.

Purpose of the Study:

  • To synthesize and evaluate two novel SMDCs targeting PSMA for metastatic prostate cancer.
  • To compare the efficacy and pharmacokinetics of a cathepsin-B-cleavable linker versus a pH-responsive phosphoramidate linker.
  • To assess the safety profile of these PSMA-targeted SMDCs.

Main Methods:

  • Modular synthesis of two PSMA-targeted SMDCs incorporating either a valine-citrulline (Val-Cit) or a phosphoramidate linker.
  • Inclusion of an irreversible PSMA-binding ligand (CTT1298) and a potent cytotoxic payload (MMAE).
  • Pharmacokinetic and efficacy studies in a PSMA(+) PC3-PIP mouse model, including toxicity and payload release assessments.

Main Results:

  • Both SMDCs demonstrated significant efficacy in a PSMA(+) PC3-PIP mouse model at 0.8 mg/kg without systemic toxicity.
  • Payload (MMAE) release was predominantly localized to tumor tissue, exceeding non-target tissues by 2-3 orders of magnitude.
  • The SMDC with the pH-responsive phosphoramidate linker (SMDC2) showed superior efficacy, achieving 100% survival and complete tumor growth inhibition in 50% of mice.

Conclusions:

  • Irreversible PSMA inhibitors combined with pH-responsive linkers represent a promising strategy for targeted prostate cancer chemotherapy.
  • This approach enables specific drug delivery to tumors, significantly reducing systemic toxicity.
  • Further development of these SMDCs holds potential for improving outcomes in metastatic prostate cancer.