文档介绍：Anti-Cancer Drugs
Overview
Introduction
Overall 5-year survival : about 40%,
Mortality: second.
Overview
Goal of treatment:
Cure
Palliation
Indications of treatment:
Neoplasms disseminate;
Supplement to surgery and radiation.
Overview
Tumor susceptibility and cell cycle
undifferentiated and rapidly dividing cells
a. cell cycle specificity
b. tumor growth rate
Overview
Cell-cycle specificity of drugs:
Cell-cycle specific drugs
Antimetabolites
Bleomycin peptide
Antibiotics
Vinca alkaloids
etoposide
Effective for high growth fraction malignancies, ., hematologic cancers
Cell-cycle non-specific drugs
Alkylating agents
Antibiotics
Cisplatin
Nitrosoureas
Effective for both low growth fraction malignacies, ., solid tumors, as well as high growth fraction malignancies
Overview
Treatment regiment and scheduling:
log kill
pharmacologic sanctuaries
Treatment protocols:
combinations of drugs;
advantages of drug combinations;
treatment protocols
Overview
Problems of chemotherapy:
Resistance
Multidrug resistance
Toxicity
ADP+Pi
ATP
Medicine
Medicine
a. common adverse effects
b. duration of adverse effects
c. minimizing adeverse effects
Antimetabolites
Folic acid Antagonists: MTX
Purine Antagonists: 6-MP
6-TG
Pyrimidine Antagonists: 5-FU
ara-C
HU
--------- S phase (cell-cycle) specific
Antimetabolites
Methotrexate (MTX)
Antimetabolites
6-Mercaptopurine (6-MP)
Site of action: inhibition of purine synthesis
Application: Acute lymphoblastic leukemia (ALL)
Adverse effects: bone marrow depression