5-fluorouracil: Difference between revisions
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'''5-fluorouracil''' is an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine, used as an [[antineoplastic agent]] but also as an immunomodulator in [[dermatology]]. | '''5-fluorouracil''' is an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine, used as an [[antineoplastic agent]] but also as an immunomodulator in [[dermatology]]. | ||
==Mechanisms of Action== | ==Mechanisms of Action== | ||
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| journal = Drug Dictionary, [[National Cancer Institute]]}}</ref> | | journal = Drug Dictionary, [[National Cancer Institute]]}}</ref> | ||
==Dermatology== | ==Dermatology== | ||
It is used topically for [[actinic keratosis]] and superficial [[basal cell carcinoma]]; these indications are approved by the [[Food and Drug Administration]]. Other applications include [[actinic gheilitis]], [[carcinoma in situ]] of the [[glans penis]], [[oral leukoplakia]] and [[radiodermatitis]]. | It is used topically for [[actinic keratosis]]<ref>{{citation | ||
| title = Actinic Keratosis | |||
| author = James M Spencer & Michelle Henry | |||
| date = 23 July 2010 | |||
| journal = Medscape | |||
| url = http://emedicine.medscape.com/article/1099775-overview | |||
}}</ref> and superficial [[basal cell carcinoma]]; these indications are approved by the [[Food and Drug Administration]]. Other applications include [[actinic gheilitis]], [[carcinoma in situ]] of the [[glans penis]], [[oral leukoplakia]] and [[radiodermatitis]]. | |||
==Oncology== | ==Oncology== | ||
Approved parenteral indications are [[colorectal cancer]], localized and metastatic [[gastric cancer]], metastatic [[breast carcinoma]], and [[pancreatic carcinoma]]. Additional uses include malignancy of the [[biliary tract]], localized [[breast carcinoma]], localized tumor of the anus, [[carcinoid syndrome]], [[bladder cancer]] malignancy, malignancy [[esophageal cancer]], [[head and neck tumor]], and [[bladder cancer]]. | Approved parenteral indications are [[colorectal cancer]], localized and metastatic [[gastric cancer]], metastatic [[breast carcinoma]], and [[pancreatic carcinoma]]. Additional uses include malignancy of the [[biliary tract]], localized [[breast carcinoma]], localized tumor of the anus, [[carcinoid syndrome]], [[bladder cancer]] malignancy, malignancy [[esophageal cancer]], [[head and neck tumor]], [[neuroendocrine carcinoma]]<ref>{{citation | ||
| title = Continuous 5-fluorouracil infusion plus long acting octreotide in advanced well-differentiated neuroendocrine carcinomas. A phase II trial of the Piemonte Oncology Network | |||
| author = Maria P Brizzi ''et al.'' | |||
| journal = BMC Cancer | year = 2009|volume =9| page =388|doi=10.1186/1471-2407-9-388 | |||
| url = http://www.biomedcentral.com/1471-2407/9/388 | |||
}}</ref> and [[bladder cancer]]. | |||
It is often used in combined chemotherapy regimens, and also in concert with [[radiotherapy]]. | |||
==References== | ==References== | ||
{{reflist}} | {{reflist|2}} | ||
Revision as of 16:34, 4 August 2010
5-fluorouracil is an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine, used as an antineoplastic agent but also as an immunomodulator in dermatology.
Mechanisms of Action
Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions. [1]
Dermatology
It is used topically for actinic keratosis[2] and superficial basal cell carcinoma; these indications are approved by the Food and Drug Administration. Other applications include actinic gheilitis, carcinoma in situ of the glans penis, oral leukoplakia and radiodermatitis.
Oncology
Approved parenteral indications are colorectal cancer, localized and metastatic gastric cancer, metastatic breast carcinoma, and pancreatic carcinoma. Additional uses include malignancy of the biliary tract, localized breast carcinoma, localized tumor of the anus, carcinoid syndrome, bladder cancer malignancy, malignancy esophageal cancer, head and neck tumor, neuroendocrine carcinoma[3] and bladder cancer.
It is often used in combined chemotherapy regimens, and also in concert with radiotherapy.
References
- ↑ "fluorouracil", Drug Dictionary, National Cancer Institute
- ↑ James M Spencer & Michelle Henry (23 July 2010), "Actinic Keratosis", Medscape
- ↑ Maria P Brizzi et al. (2009), "Continuous 5-fluorouracil infusion plus long acting octreotide in advanced well-differentiated neuroendocrine carcinomas. A phase II trial of the Piemonte Oncology Network", BMC Cancer 9: 388, DOI:10.1186/1471-2407-9-388