Hybrid Drugs: Design and Applications 2024

Dear Colleagues,

The general belief that agents modulating multiple biological targets could outperform single-target drugs has paved the way for the introduction of molecular hybridization as an efficient technique in drug discovery and development. The aim of this approach is to combine two (or more) pharmacophoric/bioactive subunits into a new, single chemical entity known as a hybrid molecule. When compared to its parent drugs, the new hybrid molecule may have higher affinity and efficacy, a modified selectivity profile with enhanced pharmacokinetic and pharmacodynamic restrictions, dual or multiple modes of action, minimized undesirable side effects, decreased drug–drug interactions, the reduced emergence or spread of drug resistance in pathogens, and a lower cost.

Trioxaquines, for example, are antimalarial hybrid drugs that are effective against multiresistant strains of Plasmodium falciparum. The antimalarial activity of its two separate precursors is limited, demonstrating the synergistic effect of their covalent binding. Palumed has prepared over 100 trioxaquines, and the trioxaquine PA1103-SAR116242 was selected as a candidate for preclinical development in 2007 in collaboration with Sanofi-Aventis. Estramustine is an anticancer drug that is a combination of a steroid and nitrogen mustard. This is an effective treatment for metastatic and/or progressive prostate cancer. Panobinostat (LBH-589) is a marketed drug used to treat multiple myeloma because it inhibits multiple histone deacetylase enzymes, causing apoptosis in malignant cells.

The major challenges present in developing new molecular hybrids that target complex diseases include selecting the correct target combination and achieving balanced activity while retaining drug-like properties. Nonetheless, hybridization is gaining popularity in academia and industry as a valuable tool for developing novel drugs for diseases such as cancer, malaria, tuberculosis, Alzheimer's, and others.

Dr. Parvesh Singh
Dr. Vipan Kumar
Dr. Shalini
Guest Editors

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• molecular hybrids
• anticancer
• neglected tropical diseases
• anti-Alzheimer
• anti-HIV