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Both compounds have a nitrile functional group that, when activated by the intestinal enzyme \u03b2\u2010glucosidases, releases hydrogen cyanide. The two compounds have been considered for a long time as alternative therapy for cancer treatment however, findings available in the literature are discordant on the real efficacy of laetrile\/amygdalin for the treatment of cancer, often highlighting a negative benefit\u2010risk ratio. In this regard, the study aimed to comprehensively analyze the scientific data on laetrile\/amygdalin, with a special emphasis on their pharmacokinetics, underlying pharmacological properties, mode of action as a potent antitumor agent, and effect on human health. The results showed that there is no clear evidence on the efficacy of cancer therapy following laetrile\/amygdalin administration, especially at the clinical trial level. However, the in vitro studies of the biological activity of these compounds showed positive effects related to their antifibrotic, anti\u2010inflammatory, antiasthmatic, and immunoregulatory processes. Laetrile's mechanism of action closely resembles amygdalin, affecting cancer signaling pathways. However, due to its cyanide toxicity, it was banned by the food and drug administration (FDA) due to safety concerns. Despite not receiving permission from the FDA, laetrile emerged as an alternative therapy in the 1970s. Nonetheless, continuing research is investigating safer methods of activating Laetrile for targeted cancer treatment. This opens interesting prospects in using these compounds in alternative medical therapies, for which, however, further research is needed.<\/jats:p>","DOI":"10.1002\/cbin.12276","type":"journal-article","created":{"date-parts":[[2025,1,28]],"date-time":"2025-01-28T10:46:07Z","timestamp":1738061167000},"page":"205-220","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["Anticancer Attributes and Multifaceted Pharmacological Implications of Laetrile and Amygdalin"],"prefix":"10.1002","volume":"49","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6382-7713","authenticated-orcid":false,"given":"Katya","family":"Carbone","sequence":"first","affiliation":[{"name":"CREA\u2010Research Centre for Olive, Fruit and Citrus Crops Rome Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4219-9292","authenticated-orcid":false,"given":"Oksana","family":"Sytar","sequence":"additional","affiliation":[{"name":"Department of Plant Biology Department Taras Shevchenko National University of Kyiv, Institute of Biology Kyiv Ukraine"},{"name":"Department of Plant Physiology Slovak University of Agriculture Nitra Slovakia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0378-8887","authenticated-orcid":false,"given":"Farukh","family":"Sharopov","sequence":"additional","affiliation":[{"name":"Research Institution \u201cChinese\u2010Tajik Innovation Center for Natural Products\u201d, National Academy of Sciences of the Republic of Tajikistan Dushanbe Tajikistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3156-2500","authenticated-orcid":false,"given":"Raffaele","family":"Pezzani","sequence":"additional","affiliation":[{"name":"Phytotherapy Lab (PhT\u2010Lab), Endocrinology Unit, Department of Medicine (DIMED) University of Padova Padova Italy"},{"name":"AIROB, Associazione Italiana per la Ricerca Oncologica di Base Padova Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7555-0486","authenticated-orcid":false,"given":"Raffaele","family":"Romano","sequence":"additional","affiliation":[{"name":"Department of Agricultural Sciences University of Napoli Federico II Portici Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5505-3327","authenticated-orcid":false,"given":"Antonello","family":"Santini","sequence":"additional","affiliation":[{"name":"Department of Pharmacy University of Napoli Federico II Napoli Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5836-4865","authenticated-orcid":false,"given":"Marek","family":"Kieliszek","sequence":"additional","affiliation":[{"name":"Department of Food Biotechnology and Microbiology, Institute of Food Sciences Warsaw University of Life Sciences\u2014SGGW Warsaw Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0005-8460-3662","authenticated-orcid":false,"given":"Tooba","family":"Khan","sequence":"additional","affiliation":[{"name":"Department of Healthcare Biotechnology, Atta\u2010ur\u2010Rahman School of Applied Biosciences (ASAB) National University of Sciences and Technology (NUST) Islamabad Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9946-9057","authenticated-orcid":false,"given":"Khushbukhat","family":"Khan","sequence":"additional","affiliation":[{"name":"Department of Healthcare Biotechnology, Atta\u2010ur\u2010Rahman School of Applied Biosciences (ASAB) National University of Sciences and Technology (NUST) Islamabad Pakistan"},{"name":"Preclinical and Clinical Department Lahore Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8575-0131","authenticated-orcid":false,"given":"Angela","family":"Caunii","sequence":"additional","affiliation":[{"name":"\u201cVictor Babes\u201d University of Medicine and Pharmacy Timisoara Timisoara Romania"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6743-2244","authenticated-orcid":false,"given":"Solomon","family":"Habtemariam","sequence":"additional","affiliation":[{"name":"Pharmacognosy Research &amp; 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