DDInter148 DDInter308
Azacitidine is a pyrimidine nucleoside analogue with anti-neoplastic activity. It differs from cytosine by the presence of nitrogen in the C5-position, key in its hypomethylating activity.[A1406,A1413,A1415] Two main mechanisms of action have been proposed for azacitidine. One of them is the induction of cytotoxicity. As an analogue of cytidine, it is able to incorporate into RNA and DNA, disrupting RNA metabolism and inhibiting protein and DNA synthesis. The other one is through the inhibition of DNA methyltransferase, impairing DNA methylation. Due to its anti-neoplastic activity and its ability to inhibit methylation in replicating DNA, azacytidine has been used mainly used in the treatment of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML), two types of cancer characterized by the presence of aberrant DNA methylation.[
Myelodysplastic syndromes (MDS) are a group of hematopoietic neoplasms that give rise to variable cytopenias progressing to secondary acute myeloid leukemia (sAML), which is invariably fatal if untreated.[A215082, A215092, A215097] Hypomethylating agents such as [decitabine] and [azacitidine] are used to treat MDS through inducing DNA hypomethylation and apoptosis of cancerous cells.[A215127, L14897] Although effective, these compounds are rapidly metabolized by cytidine deaminase (CDA) prior to reaching systemic circulation when administered orally, necessitating intramuscular or intravenous administration routes.[A215107, A215112, A215117, A215127] Cedazuridine is a fluorinated tetrahydrouridine derivative specifically designed to inhibit CDA and facilitate oral administration of hypomethylating agents.[A215107, A215112, A215117, A215127, L14897] Cedazuridine was first reported in 2014, and was subsequently approved by the FDA on July 7, 2020, in combination with [decitabine] for sale by Astex Pharmaceuticals Inc under the name INQOVI®.
Azacitidine {u} (Compound) resembles {v} (Compound) Adenosine
Azacitidine {u} (Compound) resembles {v} (Compound) S-Adenosylmethionine
Azacitidine {u} may lead to a major life threatening interaction when taken with {v} Cladribine
Azacitidine {u} (Compound) binds {v} (Gene) DNMT3A
Azacitidine {u} (Compound) upregulates {v} (Gene) FOXJ3
Azacitidine {u} (Compound) is included by {v} (Pharmacologic Class) Nucleic Acid Synthesis Inhibitors
Azacitidine {u} (Compound) downregulates {v} (Gene) ANXA2
Azacitidine {u} (Compound) causes {v} (Side Effect) Neck pain
Azacitidine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Candida albicans
Azacitidine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Efalizumab
Azacitidine (Compound) resembles Adenosine (Compound)
Azacitidine (Compound) resembles S-Adenosylmethionine (Compound)
Azacitidine may lead to a major life threatening interaction when taken with Cladribine
Azacitidine (Compound) binds DNMT3A (Gene)
Azacitidine (Compound) upregulates FOXJ3 (Gene)
Azacitidine (Compound) is included by Nucleic Acid Synthesis Inhibitors (Pharmacologic Class)
Azacitidine (Compound) downregulates ANXA2 (Gene)
Azacitidine (Compound) causes Neck pain (Side Effect)
Azacitidine may cause a moderate interaction that could exacerbate diseases when taken with Candida albicans
Azacitidine may cause a moderate interaction that could exacerbate diseases when taken with Efalizumab