NIME Next Batch PGI Quest in Delhi from 10 August to 20 August
B. 5-FU
C. Busulfan
D. Melphalan
Which antitumor drug is not an alkylating agent?
A. CyclophosphamideB. 5-FU
C. Busulfan
D. Melphalan
Ans. D.
Alkylating agents are electrophhle molecules that react with electron rich atoms to form covalent bond.
Examples: Cyclophosphamide, Ifosfamide
• Mechlorethoamine
• Dacarbazine
• Thiotepa
• Carmustine
• Chlorambudil
• Procarbazine
• Busulphan
• Temezolamide
• Cisplatin, Carboplatin and oxiliplatin
Mech. of action: These agents form reactive intermediates that covalently modify bases in DNA. In addition they can activate apoptosis.
Major site of action within DNA is N7 portion of guanine.
Alkylating agents are electrophhle molecules that react with electron rich atoms to form covalent bond.
Examples: Cyclophosphamide, Ifosfamide
• Mechlorethoamine
• Dacarbazine
• Thiotepa
• Carmustine
• Chlorambudil
• Procarbazine
• Busulphan
• Temezolamide
• Cisplatin, Carboplatin and oxiliplatin
Mech. of action: These agents form reactive intermediates that covalently modify bases in DNA. In addition they can activate apoptosis.
Major site of action within DNA is N7 portion of guanine.
Common
toxicities: Myelosuppression, alopecia, gonadal dysfunction, pulmonary
fibrosis, mucositis, second neoplasm (esp leukemia):
5-FU is an antimetabolite:
• It is a pyrimidine antagonist
• Converted in body to 5-fdUMP which inhibits thymi dylate synthetase, resulting in inhibition of DNA synthesis through: “thymine less death”
• In addition it gets incorporated into RNA causing single stranded break.
Toxicity: Mucositis, Diarrhoea, Myebosuppression, Hand foot syndrome.
5-FU is an antimetabolite:
• It is a pyrimidine antagonist
• Converted in body to 5-fdUMP which inhibits thymi dylate synthetase, resulting in inhibition of DNA synthesis through: “thymine less death”
• In addition it gets incorporated into RNA causing single stranded break.
Toxicity: Mucositis, Diarrhoea, Myebosuppression, Hand foot syndrome.
