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Introduction to chemotherapy agents
Dr. V. S. Swathi
Assistant Professor
Chemotherapy agents
These are the drugs which are used in treatment of cancer
Types
– Alkylating agents
– Antitumor antibiotics
– Antimetabolites
– Mitotic inhibitors
– Topoisomerase inhibitors
– Enzymes
– Protein tyrosine kinase inhibitors
– Miscellaneous agents
Modeofaction
Alkylating agents
Examples
• Busulfan
• Carboplatin
• Cisplatin
• Oxaliplatin
• Cyclophosphomide
• Ifosfamide
Adverse effects
• Myelosupression
• Peripheral neuropathy
• Nephrotoxicity
• Ototoxicity
• Alopecia
Mode of action
These are phase non specific
agents
These acts by cross linking and
abnormal base pairing of DNA
strands which inhibit replication of
DNA and inhibits cancer cell
production (Alkylation)
Indications
• Leukaemia
• Lymphoma
• Hodgkins disease
• Multiple myeloma
• Sarcoma
Antitumor antibiotics
Examples
• Bleomycin
• Doxorubicin
• Epirubicin
Adverse effects
• Myelosupression
• Cardiotoxicity
• Stomatitis
• Alopecia
• Nausea and Vomiting
Mode of action
These are phase non specific
agents
These acts by sliding between
DNA base pairs and inhibit
synthesis of DNA and inhibits
cancer cell production
(Intercalation)
Indications
• Cancer of bladder, breast and
bone
• Other cancers
Antimetabolites
Examples
• Cytarabine
• Fluorouracil
• Methotrexate
• Mercaptopurine
• Gemcitabine
Adverse effects
• Myelosupression
• Hepatotoxicity
• Nephrotoxicity
• Stomatitis
• Mucositis
Mode of action
These are S phase specific agents
These acts by acting as false
substitutions in the production of
nucleic acids
Indications
• Leukaemia
• Cancer of GIT, breast and ovary
Antitumor antibiotics
Examples
• Bleomycin
• Doxorubicin
• Epirubicin
Adverse effects
• Myelosupression
• Cardiotoxicity
• Stomatitis
• Alopecia
• Nausea and Vomiting
Mode of action
These are phase non specific
agents
These acts by sliding between
DNA base pairs and inhibit
synthesis of DNA and inhibits
cancer cell production
(Intercalation)
Indications
• Cancer of bladder, breast and
bone
• Other cancers
Mitotic inhibitors
Examples
• Paclitaxel
• Vincristine
Adverse effects
• Myelosupression
• Fluid retention
• Peripheral neuropathy
• Alopecia
• Mucositis
Mode of action
These are M phase specific agents
These acts by arresting cell division
by preventing microtubules
Indications
• Myeloma
• Lymphoma
• Leukaemia
• Cancer of lung and breast
Topoisomerase inhibitors
Examples
• Etopside
Adverse effects
• Myelosupression
• Hypotension
• Alopecia
• Nausea and vomiting
• Diarrhea
Mode of action
These are G2 phase specific
agents
These acts by inhibiting
Topoisomerase enzyme which is
involved in DNA replication and
RNA transcription
Indications
• Leukaemia
• Cancer of GIT, breast and ovary
Examples
• Aspariginase
Adverse effects
• Allergic reactions
• Nausea and vomiting
• Liver dysfunction
• CNS depression
• Hyperglycaemia
Mode of action
These are G1 phase specific
agents
It acts by breaking asparigine there
by no proteins are available for
cancer cell production
Indications
• Leukaemia
• Non Hodgkin’s lymphoma
Enzymes
Examples
• Imatinib
• Nilotinib
Adverse effects
• Myelosupression
• Hepatotoxicity
• Fluid retention
• Nausea and vomiting
• Diarrhea
Mode of action
These are target agents
These acts by causing apoptosis
and arrest the cancer cell growth
Indications
• Liver carcinoma
• Renal carcinoma
• Prostatic cancer
• Leukaemia
• Lymphoma
Protein tyrosine kinase inhibitors
Miscellaneous agents
Retinoic acid derivatives
– Tretinoin
– Isotretinoin
Arsenic trioxide
Bortezomib
Thalidomide
Hormones
Biological response modifiers
– Cytokines
Monoclonal antibodies
– Rituximab
– Trastuzumab

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Chemotherapy agents

  • 1. Introduction to chemotherapy agents Dr. V. S. Swathi Assistant Professor
  • 2. Chemotherapy agents These are the drugs which are used in treatment of cancer Types – Alkylating agents – Antitumor antibiotics – Antimetabolites – Mitotic inhibitors – Topoisomerase inhibitors – Enzymes – Protein tyrosine kinase inhibitors – Miscellaneous agents
  • 4. Alkylating agents Examples • Busulfan • Carboplatin • Cisplatin • Oxaliplatin • Cyclophosphomide • Ifosfamide Adverse effects • Myelosupression • Peripheral neuropathy • Nephrotoxicity • Ototoxicity • Alopecia Mode of action These are phase non specific agents These acts by cross linking and abnormal base pairing of DNA strands which inhibit replication of DNA and inhibits cancer cell production (Alkylation) Indications • Leukaemia • Lymphoma • Hodgkins disease • Multiple myeloma • Sarcoma
  • 5. Antitumor antibiotics Examples • Bleomycin • Doxorubicin • Epirubicin Adverse effects • Myelosupression • Cardiotoxicity • Stomatitis • Alopecia • Nausea and Vomiting Mode of action These are phase non specific agents These acts by sliding between DNA base pairs and inhibit synthesis of DNA and inhibits cancer cell production (Intercalation) Indications • Cancer of bladder, breast and bone • Other cancers
  • 6. Antimetabolites Examples • Cytarabine • Fluorouracil • Methotrexate • Mercaptopurine • Gemcitabine Adverse effects • Myelosupression • Hepatotoxicity • Nephrotoxicity • Stomatitis • Mucositis Mode of action These are S phase specific agents These acts by acting as false substitutions in the production of nucleic acids Indications • Leukaemia • Cancer of GIT, breast and ovary
  • 7. Antitumor antibiotics Examples • Bleomycin • Doxorubicin • Epirubicin Adverse effects • Myelosupression • Cardiotoxicity • Stomatitis • Alopecia • Nausea and Vomiting Mode of action These are phase non specific agents These acts by sliding between DNA base pairs and inhibit synthesis of DNA and inhibits cancer cell production (Intercalation) Indications • Cancer of bladder, breast and bone • Other cancers
  • 8. Mitotic inhibitors Examples • Paclitaxel • Vincristine Adverse effects • Myelosupression • Fluid retention • Peripheral neuropathy • Alopecia • Mucositis Mode of action These are M phase specific agents These acts by arresting cell division by preventing microtubules Indications • Myeloma • Lymphoma • Leukaemia • Cancer of lung and breast
  • 9. Topoisomerase inhibitors Examples • Etopside Adverse effects • Myelosupression • Hypotension • Alopecia • Nausea and vomiting • Diarrhea Mode of action These are G2 phase specific agents These acts by inhibiting Topoisomerase enzyme which is involved in DNA replication and RNA transcription Indications • Leukaemia • Cancer of GIT, breast and ovary
  • 10. Examples • Aspariginase Adverse effects • Allergic reactions • Nausea and vomiting • Liver dysfunction • CNS depression • Hyperglycaemia Mode of action These are G1 phase specific agents It acts by breaking asparigine there by no proteins are available for cancer cell production Indications • Leukaemia • Non Hodgkin’s lymphoma Enzymes
  • 11. Examples • Imatinib • Nilotinib Adverse effects • Myelosupression • Hepatotoxicity • Fluid retention • Nausea and vomiting • Diarrhea Mode of action These are target agents These acts by causing apoptosis and arrest the cancer cell growth Indications • Liver carcinoma • Renal carcinoma • Prostatic cancer • Leukaemia • Lymphoma Protein tyrosine kinase inhibitors
  • 12. Miscellaneous agents Retinoic acid derivatives – Tretinoin – Isotretinoin Arsenic trioxide Bortezomib Thalidomide Hormones Biological response modifiers – Cytokines Monoclonal antibodies – Rituximab – Trastuzumab