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Anticancer drugs 5 targeted drugs

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Anticancer drugs 5 targeted drugs

  1. 1. Anticancer drugs Dr. S. Parasuraman Faculty of Pharmacy, AIMST.
  2. 2. Classification of anticancer agents Targeted drugs 1. 2. 3. 4. 5. Tyrosine proteinkinase inhibitors: Imatinib, Nilotinib EGF receptor inhibitor: Gefitinib, Erlotinib Angiogenesis inhibitors: Bevacizumab Proteasome inhibitor: Bortezomib Unarmed monoclonal antibody: Rituximab, Trastuzumab
  3. 3. Classification of anticancer agents Hormonal drugs 1. 2. 3. 4. 5. 6. 7. 8. 9. Glucocorticods: Prednisolone Estrogens: Fosfestrol, ethinylestradiol Selective estrogen receptor modulators: Tamoxifen Selective estrogen receptor down-regulators: Fulvestrant Aromatase inhibitors: Letrozole, Anastrozole Antiandrogen: Flutamide 5-α reductase inhibitor: Finasteride GnRH analogues: Nafarelin, Triotorelin Progestins: Hydroxyprogesterone acetate
  4. 4. Tyrosine proteinkinase inhibitors Imatinib: • Imatinib is a novel antineoplastic drug which inhibits the tyrosine protein kinases in chronic myeloid leukaemia (CML) cells. • Used for the treatment of CML in blast crisis as well as GI stromal tumor. • Pharmacokinetics: The drug is very well absorbed orally. It undergoes metabolism by the CYP450 system to several compounds, of which the N-demethyl derivative is active. Excretion is predominantly through feces. • Adverse effects are fluid retention, edema, vomiting, abdominal pain, myalgia , liver damage, hepatotoxicity, and thrombocytopenia or neutropenia. • Dose: 400 mg/day with meal; accelerated phase of CML 600-800 mg/day.
  5. 5. EGF (epidermal growth factor receptor) receptor inhibitor Gefitinib: • It is approved for the treatment of non–small cell lung cancer. • Gefitinib is usually used as a single agent. • PK: Oral administration. Metabolism in the liver by the CYP450 enzyme CYP3A4 and excreted through feces. • The most common adverse effects are diarrhea, nausea, and acne-like skin rashes. A rare but potentially fatal adverse effect is interstitial lung disease, which presents as acute dyspnea with cough.
  6. 6. Unarmed monoclonal antibody Rituximab: • Rituximab is a chimeric monoclonal antibody against, which is primarily surface the immune system B cells. • Pharmacokinetics: Rituximab is administered as two 1000-mg IV infusions separated by 2 weeks. To reduce the severity of infusion reactions, methylprednisolone at 100 mg IV or its equivalent is administered 30 minutes prior to each infusion. The mean terminal elimination half-life after the second dose is 19 days. • Adverse effects: Infusion reactions (that is, urticaria, hypotension, and angioedema) are the most common complaints with this agent and typically occur during the first infusion. If the infusion is to be continued, then the rate of infusion should be reduced by 50 percent after symptoms have completely resolved. Others: Cardiac arrest, cytokine release syndrome , tumor lysis syndrome and causing acute renal failure. • Use: Hematological cancers, autoimmune diseases and anti-rejection treatment for organ transplants.
  7. 7. Aromatase inhibitors Letrozole, Anastrozole: • They have gained favor in the treatment of breast cancer because – – – – – they are more potent they are more selective than aminoglutethimide they do not need to be supplemented with hydrocortisone they do not predispose to endometrial cancer they are devoid of the androgenic side effects that occur with the steroidal aromatase inhibitors • Use: first-line drugs in other countries for the treatment of breast cancer
  8. 8. Hormonal drugs Drug Use Glucocorticods: Prednisolone • primarily used in acute childhood leukaemia and lymphomas Estrogens: Fosfestrol, ethinylestradiol They produce symptomatic relief in carcinoma prostate which is an androgen-dependent tumour. Selective estrogen receptor modulators: Tamoxifen • Estrogen antagonist • Used for firstline therapy in the treatment of estrogen receptor–positive breast cancer. • Approved only for 5 years of use. • PK: orally effective, metabolized in liver, excreted through the bile into the feces ADR Hot fl ashes, nausea, vomiting, skin rash and vaginal bleeding. Tamoxifen has the potential to cause endometrial cancer.
  9. 9. Hormonal drugs Drug Use Aromatase inhibitors: Letrozole, • Prevent relapse of breast cancer after Anastrozole partial mastectomy and radiation therapy Antiandrogen: Flutamide palliative effect in advanced/metastatic cases Wont cause bone marrow depression GnRH analogues: Nafarelin, Triotorelin Indirectly inhibit estrogen/ androgen secretion by suppressing FSH and LH release from pituitary and have palliative effect in advanced estrogen/ androgen dependent carcinoma breast/prostate. Progestins: Hydroxyprogesterone acetate Temporary remission in some cases of advanced, recurrent (after surgery /radiotherapy) and metastatic endometrial carcinoma
  10. 10. Thank you

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