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. 2021 Feb 22;3(8):2157–2179. doi: 10.1039/d0na01084g

A list of FDA and EMA approved chemotherapeutic nucleosidic analogs.

Name Structure Statusa Chemical modification Targeted cancer Mechanism of action
Fluorouracil graphic file with name d0na01084g-u1.jpg FDA approved (1962) • Uracil modification by F-halogenation • Colon, esophageal, stomach, pancreatic, breast, and cervical cancers • Enzymatic inhibition 37
EMA approved (NA)
Floxuridine graphic file with name d0na01084g-u2.jpg FDA approved (1970) • Cytosine modification by F-halogenation • Colon cancer • Enzymatic inhibition 38
• DNA synthesis inhibition
Cytarabine graphic file with name d0na01084g-u3.jpg FDA approved (1969) • Replacement of the ribose sugar ring with an arabinose • Acute myelogenous leukemia • DNA polymerase inhibition 5
EMA approved (2001) • Lymphoblastic leukemia
Gemcitabine graphic file with name d0na01084g-u4.jpg FDA approved (1996) • Sugar ring F-halogenation • Pancreatic, lung, breast, and bladder cancers • Enzymatic inhibition 7
EMA approved (2008)
Azacitidine graphic file with name d0na01084g-u5.jpg FDA approved (2004) • Cytosine modification by azotation • Myelodysplastic syndromes (MDS) • DNA hypomethylation 39
EMA approved (2008) • Acute myeloid leukemia (AML)
Decitabine graphic file with name d0na01084g-u6.jpg FDA approved (2006) • Cytosine modification by azotation • Myelodysplastic syndromes (MDS) • DNA hypomethylation 6
EMA approved (2006) • Acute myeloid leukemia (AML)
Cladribine graphic file with name d0na01084g-u7.jpg FDA approved (1993) • Adenine modification by Cl-halogenation • Hairy-cell leukemia • Enzymatic depletion 40
EMA approved (2004) • Non-Hodgkin lymphoma • ATP accumulation
Fludarabine graphic file with name d0na01084g-u8.jpg FDA approved (1991) • Adenine modification by F-halogenation • Chronic lymphocytic leukemia • Nucleic acid synthesis inhibition 41
EMA approved (2014) • Replacement of the ribose sugar ring with an arabinose • Enzymatic inhibition
Nelarabine graphic file with name d0na01084g-u9.jpg FDA approved (2005) • Guanine by modification of a functional group • T-cell acute lymphoblastic leukemia and lymphoma • DNA synthesis inhibition 42
• Sugar ring is an arabinose instead of ribose
a

Approval status was verified by the European Medicines Agency (http://www.ema.europa.eu) and the US Food and Drug Administration (http://www.fda.gov).