Prodrug Strategies in Cancer Chemotherapy
Summary
Prodrug design in cancer chemotherapy encompasses the synthesis of inert precursors that undergo selective conversion into cytotoxic agents within the tumour milieu. Such strategies aim to enhance therapeutic index by improving drug solubility, stability and tumour selectivity while minimising systemic toxicity. Activation mechanisms commonly exploit endogenous tumour characteristics, including elevated enzymatic activity (for example β-glucuronidase, cathepsin B or matrix metalloproteinases), altered pH or redox potential. In addition, ligand-mediated targeting employs conjugation of cytotoxins to sugars, peptides or proteins that bind receptors overexpressed on cancer cells, thereby improving uptake and residence time. Nanocarriers, such as polymeric micelles or nanogels, further refine prodrug performance by shielding payloads during circulation and releasing them in response to defined stimuli. Collectively, these approaches address longstanding challenges in conventional chemotherapy by directing active agents selectively to malignant tissue, overcoming multidrug resistance and allowing dose intensification with reduced off-target effects. The global significance of prodrug technologies is underscored by their versatility, with applications spanning solid tumours, haematological malignancies and combination regimens integrating radiotherapy or immunotherapy.
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Prodrug Strategies in Cancer Chemotherapy publication trend
The graph below shows the total number of articles in prodrug strategies in cancer chemotherapy across all publications each year (not limited to Nature Index journals).
Technical terms
Prodrug: A pharmacologically inactive precursor that is biochemically converted to an active drug within the body.
Tumour microenvironment: The complex milieu surrounding cancer cells, characterised by unique pH, enzymatic profiles and cellular components.
β-Glucuronidase: An enzyme overexpressed in many tumours that cleaves glucuronide linkages to release active agents.
Glycosylation: The attachment of sugar moieties to drugs or carriers to enhance solubility and target cell uptake.
Nanogel: A nanoscale hydrogel network capable of encapsulating prodrugs and releasing them in response to specific stimuli.
References
- A Small Sugar Molecule with Huge Potential in Targeted Cancer Therapy. Pharmaceutics (2023).
- Chloromethyl Glycosides as Versatile Synthons to Prepare Glycosyloxymethyl‐Prodrugs. Chemistry - A European Journal (2022).
- Clathrin light chain‐conjugated drug delivery for cancer. Bioengineering & Translational Medicine (2022).
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