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CYTARABINE Ferdinand F. Fatiga, RMT

Cytarabine

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CYTARABINE (Chemotherapy Drug)

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CYTARABINE

Ferdinand F. Fatiga, RMT

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CYTARABINE

• Used in the treatment of WBC cancers (AML/ALL) and Lymphoma

• Antimetabolite

• S-Phase-specific Chemotherapy drug

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CYTARABINE

• Ara-C / Cytosine Arabinoside

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CYTIDINE• Cytosine normally combines

with Ribose / Deoxyribose sugar

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CYTARABINE vs. CYTIDINE

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CYTARABINE (Mechanism of Action)

Nucleoside Transporter

dCK

Deoxycytidylate Kinase

NDK

Nucleotidase 1

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CYTARABINE (Mechanism of Action)

MDR (P-glycoprotein)

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CYTARABINE (Mechanism of Action)

Cytidine Deaminase

Deoxycytidylate Deaminase

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CYTARABINE TRIPHOSPHATE

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ACTION MODE OF araCTP

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CYTARABINECytarabine is converted to its activated

Triphosphate form

Upon incorporation into DNA, the Cytidine analog interferes with chain elongation and promotes abnormal fragment ligation of newly synthesized DNA

If araCTP ends up being incorporated into DNA, it leads to Apoptosis

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CONCLUSIONParameters in araC Sensitivity

Conversion to Triphosphate activated form by Kinases Inactivation via Deamination Overexpression of MDR transporters Half-life of active form araCTP

Increased expression of MDR such as P-glycoprotein and enzymes (Deaminases) that counteract the activation of araC to its activated araCTP cause cancer tumor cell resistance.

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Thank you!

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