Masood 1 Salaar Masood Amir Faisal BIO 101 7 May 2023 Oral Chemotherapeutic drugs: its History and Development as a cancer treatment. Chemotherapy is a widely recognized treatment for cancer, and recent advances in science have now led to the development of oral chemotherapeutic drugs. These drugs offer the potential for increased convenience and improved quality of life for patients, as it helps them get the required treatment in the comfort of their homes. Despite the potential benefits, however, scientists have encountered numerous challenges and obstacles during the development of oral chemotherapeutic drugs, including low bioavailability, gastrointestinal toxicity, and patient adherence. One primary challenge in developing oral chemotherapeutic drugs is ensuring adequate bioavailability. Bioavailability refers to the extent to which a drug is absorbed by the body and becomes available at the target site to produce its intended therapeutic effect. According to Eisenmann et al., anticancer drugs often have limited bioavailability due to physicochemical and physiological limitations. These limitations effectively reduce the drug's ability to kill cancer cells, as a higher dose might be needed to achieve the same therapeutic effect. Consequently, this could increase the risks of side effects associated with chemotherapy. An alternative approach involves the development of prodrugs, which are biologically inactive compounds that convert into active drugs once inside the body (Kratz et al.), but such strategies often require extensive Masood 2 research and development, leading to increased overall costs and time required for drug development. Furthermore, gastrointestinal toxicity presents a significant challenge for scientists developing oral chemotherapeutic drugs. Many chemotherapeutic drugs can cause severe side effects in the GI tract, such as nausea, vomiting, diarrhea, and mucositis (Carr et al.). These side effects can lead to dose reductions or therapy termination, as well as a loss in therapeutic efficacy. In addition, the GI tract serves as a major barrier to oral drug absorption, and damage to the GI mucosa can further decrease the bioavailability of the administered drug. To reduce GI toxicity, researchers have been developing targeted drug delivery systems that can address issues of anti-cancer drug solubility and chemical stability, protect anti-cancer compounds from biodegradation or excretion, and deliver the chemotherapeutic drug specifically to the tumor site (Wicki et al.). However, developing such targeted drug delivery systems is complex and requires a thorough understanding of the tumor microenvironment and drug release kinetics. Lastly, patient adherence to oral chemotherapeutic drugs can pose a significant challenge. While oral administration offers greater convenience and flexibility, it also places responsibility on patients for their treatment, potentially leading to non-adherence due to forgetfulness, misunderstanding of instructions, or intentional non-compliance. According to Given et al., "Suboptimal adherence to oral antineoplastic agents is a significant clinical problem that may result in disease or treatment complications, adjustment in treatment regimen, disease progression, and premature death." Consequently, non-adherence to oral chemotherapy can compromise treatment outcomes and increase the risk of drug resistance. In conclusion, the development of oral chemotherapeutic drugs offers several advantages over traditional intravenous administration. However, challenges such as poor bioavailability, Masood 3 gastrointestinal toxicity, and patient adherence must be overcome to fully realize oral chemotherapy's potential benefits. Innovative strategies such as the use of prodrugs and targeted drug delivery are being explored to address these challenges. Furthermore, improved patient education and adherence monitoring can also help ensure the success of oral chemotherapy regimens. Masood 4 Works Cited Carr, Craig L., et al. “The Side Effects of Chemotherapeutic Agents.” Current Anaesthesia & Critical Care, vol. 19, no. 2, Churchill Livingstone, Apr. 2008, pp. 70–79. https://doi.org/10.1016/j.cacc.2008.01.004. Eisenmann, Eric D., et al. “Boosting the Oral Bioavailability of Anticancer Drugs Through Intentional Drug–drug Interactions.” Basic & Clinical Pharmacology & Toxicology, vol. 130, no. S1, Wiley-Blackwell, Jan. 2022, pp. 23–35. https://doi.org/10.1111/bcpt.13623. Given, Barbara A., et al. “The Challenges of Oral Agents as Antineoplastic Treatments.” Seminars in Oncology Nursing, vol. 27, no. 2, Elsevier BV, May 2011, pp. 93–103. https://doi.org/10.1016/j.soncn.2011.02.003. Kratz, Felix, et al. “Prodrug Strategies in Anticancer Chemotherapy.” ChemMedChem, vol. 3, no. 1, Wiley, Jan. 2008, pp. 20–53. https://doi.org/10.1002/cmdc.200700159. Wicki, Andreas, et al. “Nanomedicine in Cancer Therapy: Challenges, Opportunities, and Clinical Applications.” Journal of Controlled Release, vol. 200, Elsevier BV, Feb. 2015, pp. 138–57. https://doi.org/10.1016/j.jconrel.2014.12.030.
