Ancitabine hydrochloride is a white needle-like crystal or crystalline powder that is freely soluble in water, slightly soluble in methanol and ethanol, and almost insoluble in ether, benzene and chloroform. The chemical name of it is 2-methanolyl 2,3,3a,9a-tetrahydro-3hydroxy-6-imino-6H furan-(2',3',4,5)-oxazole(3,2a) pyrimidine hydrochloride. Ancitabine hydrochloride is the hydrochloride salt of a cytarabine congener prodrug, so it has similar antineoplastic activity to cytarabine. It is widely used in chemotherapy for treating white blood cell cancers, especially acute myeloid leukemia (AML). The structure of ancitabine hydrochloride is shown in fig. 1.
Fig. 1 Structure of ancitabine hydrochloride
AML is a heterogeneous hematologic malignancy characterized by the clonal expansion of myeloid blasts in the peripheral blood, bone marrow, and other tissues. It is the most common form of acute leukemia in adults, accounting for about 80% of cases in acute leukemias. In the United States, the incidence of AML ranges from three to five cases per 100000 population. In 2015 alone, an estimated 20830 new cases were diagnosed, and over 10000 patients died from this disease. The incidence of AML increases with age, from 1.3 cases per 100000 population in patients under 65 years old to 12.2 cases per 10 000 population in those over 65 years old[1]. Environmental factors that have long been established to increase the risk of AML, which include prolonged exposure to petrochemicals, solvents, pesticides, and ionizing radiation.
Upon administration, ancitabine hydrochloride is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted into cytosine arabinoside triphosphate, which damages DNA when the cell cycle holds in the S phase (synthesis of DNA). Thus, the mechanism of action of ancitabine hydrochloride in AML is similar to cytarabine. Compared to cytarabine, the therapeutic effect of ancitabine hydrochloride may be longer because of the slow hydrolytic conversion of ancitabine hydrochloride to cytarabine.
Common side effects of ancitabine hydrochloride mainly include:
Leukopenia
Thrombocytopenia
Aplastic anemia
Bone marrow suppression
Megaloblastic anemia
Less common side effects of ancitabine hydrochloride mainly include:
Stomatitis
Febrile reaction
Nasal mucosal swelling
Esophagitis
Parotid gland pain
Abnormal liver function
Thrombophlebitis
Orthostatic hypotension
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