Download ANTINEOPLASTIC AGENTS

LECTURE 9 B
ANTINEOPLASTIC AGENTS
PHARMACOLOGY
OBJECTIVE
• To cause a lethal lesion that can arrest tumor’s
progression.
• The attack is generally against the metabolic sites
that are essential for cell replication.
• Ideally, only malignant cells should be targeted.
• However, currently no such drugs are available
that specifically recognize neoplastic cells,
resulting in the appearance of adverse drug
reactions (ADRs).
CLASSIFICATION
•
•
•
•
•
•
Antimetabolites
Antibiotics
Alkylating agents
Microtubule inhibtors
Steroids
Others
ANTIMETABOLITES
• Methotrexate, mercaptpurine
• Act at S phase of the cell cycle
• They inhibit the synthesis of nucleotides by
altering various genetic mechanisms
• Used in leukemia, lymphoma, inflammatory
diseases.
• ADRs: Neurological, renal, hepatic, pulmonary,
resistance.
METHOTREXATE MOA
Mercaptopurine MOA
ANTIBIOTICS
• Dactinomycin , Bleomycin, Daunorubicin,
Doxorubicin
• Interaction with DNA, leading to disruption of
DNA function
• Usually in combination with other anticancer
agents
• Choriocarcinoma, Breast, lung, leukemia,
lymphoma
• ADRs: Same as for antimetabolites plus skin
reactions and immunosuppression
ALKYLATING AGENTS
• Cyclophophamide, nitrosoureas (carmustine)
• Covalently binding to nucleophilic groups on
the DNA. Resulting in the disruption of cell
growth
• Used in lymphomas, leukemias and solid
tumors
• Same as above plus nausea, latent viral
infections (why?), alopecia, neutropenia.
MICROTUBULE INHIBITORS
•
•
•
•
Vincristine, vinblastine, paclitaxel
Act on the spindle fibers to halt cell division
The most commonly used anticancer agents.
Lekemia, lymphoma, soft and hard tissue
tumors.
• ADRs: Same as above plus neuropathy (ataxia,
foot drop)
STEROIDS
• Prednisone, tamoxifen, estrogens
• Only good for hormone responsive tumors
• Breast, ovarian, prostatic (plus sometimes in
addition to other agents for decreasing
inflammation)
• ADRs: Same as above
OTHERS
• Cisplatin – similar to alkylating agents
• Carbaplatin - similar to alkylating agents
• Etoposide – irreversible DSBs (double
stranded breaks)
• Interferons – active against tumor cells by
initiating immune response against them.
THANK YOU