Upload
ferdie-fatiga
View
302
Download
1
Embed Size (px)
DESCRIPTION
CYTARABINE (Chemotherapy Drug)
Citation preview
CYTARABINE
Ferdinand F. Fatiga, RMT
CYTARABINE
• Used in the treatment of WBC cancers (AML/ALL) and Lymphoma
• Antimetabolite
• S-Phase-specific Chemotherapy drug
CYTARABINE
• Ara-C / Cytosine Arabinoside
CYTIDINE• Cytosine normally combines
with Ribose / Deoxyribose sugar
CYTARABINE vs. CYTIDINE
CYTARABINE (Mechanism of Action)
Nucleoside Transporter
dCK
Deoxycytidylate Kinase
NDK
Nucleotidase 1
CYTARABINE (Mechanism of Action)
MDR (P-glycoprotein)
CYTARABINE (Mechanism of Action)
Cytidine Deaminase
Deoxycytidylate Deaminase
CYTARABINE TRIPHOSPHATE
ACTION MODE OF araCTP
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
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.
Thank you!