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Classification of Neoplasm
Benign
Potentially malignant
Malignant
Warning Signs of
Neoplasm
Purine Antagonist
e.g.: 6-Mercaptopurine, 6-thiogunine, Azathioprine
Pyrimidine Antagonist
e.g.: 5-Fluorouracil, Cytarabine
Vinka Alkaloids
e.g.: Vincristine, Vinblastine
Taxanes
e.g.: Paclitaxel
Epipodophyllotoxin
e.g.: Etoposide
Antibiotics
e.g.: Actinomycin, Doxorubicin, Daunorubicin,
Mitoxantrone, Bleomycins, Mithramycin.
Miscellaneous
e.g.: Hydroxyurea, Procarbazine,
L- Asparaginase, Cisplatin, Carboplatin.
Drug Altering Hormonal
milieu
•Glucocorticoids
e.g. : Prednisolone & Its Derivatives
•Estrogen
e.g.: Fosfestrol, Ethinylestradiol
•Antiestrogen
e.g.: Tomoxifen
•Antiandrogen
e.g.: Flutamide
•5 reductase inhibitor
e.g.: Finasteride
•GnRH analogues
e.g.: Naferelin, Goserelin
according to mechanism of
action
• Drugs affecting biosynthesis of nucleic acid
• Drugs destroying DNA structure and function
•Drugs interfering with transcription and blocking
RNA synthesis
• Drugs affecting protein synthesis
• Hormonal agents
Drug Affecting Nucleic Acid
Synthesis
Hydroxyurea
Drug Destroying DNA Structure
& its Function
Alkylating Agent
Camptothecins
Antitumor Antibiotics
Cisplatin &
carboplantin
Drugs interfering with
transcription
Dactinomycin
Doxorubicin
Daunorubicin
R R R R
Thiotepa( TSPA)
•It is a Ethylenimine
•Clinical uses: breast cancer, ovarian cancer, liver
cancer etc
•Toxicity: myelosuppression
•Dose: 0.3-0.4 mg/kg i.v.at 1-4 week interval
•Generic: Thiotepa 15 mg per vial inj
Busulfan (myleran)
•Good effect on chronic granulocytic leukemia
•Toxicity: myelosuppression
Nitrosourea
•Drugs : Carmustine, Lomustine
•Highly lipid-soluble, can cross BBB
•Treatment of brain tumor
•Dose: 100-130 mg orally
•Branded Name: Lomustine 40, 100 mg cap.
Azathioprine:
Effects on T lymphocytes & suppress CMI
Use : immunosuppressant in organ transplantation & in
rheumatoid arthritis
Dose: 3-5 mg/kg/day
Pyrimidine antagonists
Fluorour acil ( 5-Fu )
Mechanism: convert to 5F-dUMP and inhibit thynidylate
synthase,block the synthesis of dTMP
Clinical uses: good effect on cancer of digestive tract, breast cancer
Toxicity : myelosuppression and mucositis
Dose: 1 gm orally on alternative days.
Branded Name: Fluracil, five fluro250 mg cap, 5 ml for i.v. inj.
Cytarabine ( Ara- C )
Ara-C →Ara-CMP →→Ara-CTP, competitively inhibit DNA
polymerase. The triphosphate of Cytarabine is an inhibitor of
DNA polymerase.
Clinical uses: acute granulocytic leukemia, mononuclearcyte
leukemia
Toxicity: severe myelosuppression , nausea etc
Dose: 1.5-3 mg/kg i.v. BD for 5-10 days
Branded Name: Cytarabine, cytosar & cytabin 100, 500, 1000 mg inj.
Vinka Alkaloids
Mechanism of action
Vinblastin:
• Use :in Hodgkin's disease & testicular carcinoma.
• Dose: 0.1-0.15 mg/kg
• Generic: Vinblastin 10 mg/vial inj
• Toxicity
VLB: nausea, vomiting, alopecia, myelosuppression
VCR: neurotoxicity , include muscle weakness,
peripheral neuritis and are flexia
Taxanes
Paclitax al
•Mechanism: Enhance tubulin polymerization and promote
microtubule assembly
•Clinical uses: First choice for ovarian and advanced breast cancer
•Toxicity : Hypersensitivity, Peripheral neuropathy, Neutropenia ,
thrombocytopenia
•Dose: 175 mg by i.v. infusion over 3 hr, repeated every 3 weeks.
•Branded Name: Intaxel, paxtal 30 mg in 5 ml cremophor emulsion.
Docetaxel:
•More potent then Paclitaxel
•Use: breast & ovarian cancer. Also in gastric & head, neck carcinoma.
•Dose: 100 mg i.v over 1 hr repeat at 3 weeks
•Branded Name: Daxotel 20 mg, 80 mg inj.
Epipodophyllotoxin
Etoposide:
Semi synthetic derivative of podophyllotoxin. It arrest the
cells in G2 phase & cause the DNA breaks by affecting the
DNA topoisomerase II function .
Use: testicular tumor, lung cancer, Hodgkin's disease.
Dose: 50-100 mg /day oral for 5 days.
Branded Name: Peltasol 100 mg in 5 ml inj.
Camptothecin Analogues
Topotecan & Irinotecan are two semi synthetic analogues of Camptothecin.
They act similar as Etoposide but interact with different enzyme
topoisomerase I .
Topotecan:
Use: In metastatic carcinoma of ovary & small cell lung cancer.
AE: pain abdomen, vomiting & diarrhea
Dose: 1.5 mg i.v. over 30 min daily for 5 days.
Branded Name : Topotel 2.5 mg & 4.0 mg inj
Irinotecan:
It produces the cholinergic effects because it inhibit the AChE.
Use : Colorectal carcinoma, cancer lung/cervix/ovary
AE: body ach, weakness.
Dose: 125 mg i.v. over 90 min weekly for 4 weeks
Branded Name: Irinotel 40 mg, 100 mg inj.
Antibiotics
Dactinomycin
• Mechanism: bind tightly to double-stranded DNA
through interaction between adjacent guanine-
cytosine base pair, and inhibit all forms of DNA-
dependent RNA synthesis
• Clinical uses: narrow-spectrum
In combination with surgery and Vincristine in
the adjuvant treatment of Wilm’s tumor
• Toxicity : evident myelosuppression
• Dose: 15 g/kg i.v. daily for 5 days.
• Branded Name: 0.5 mg/vial inj.
Doxorubicin & Daunorubicin:
• Mechanism : Bind with high affinity to DNA through
intercalation and then block the synthesis of DNA and
RNA
• Clinical uses
ADM: one of the most important anticancer drugs ,
treatment of carcinoma of the breast, endometrium,
ovary, testicle, thyroid, lung and many sarcoma,
acute leukemia, Hodgkin’s disease
Daunorubicin: acute leukemia
• Dose: Doxorubicin 60-75 mg slow i.v. inj. every 3
weeks.
• Daunorubicin: 30-60 mg daily for 3 days repeat
weekly.
• Branded Name: Daunocin 20 mg/vial inj
• Adrimycin Doxorubicin Oncodria 10 mg, 50 mg per
vial inj.
Mitox antrone :
• It is a analogue of doxorubicin
• Use : chronic myelogenous leukemia, non
Hodgkin’s lymphoma & carcinoma breast.
Bleomycin:
• It is mixture of glycopeptides antibiotics having anti
tumor activity.
• Dose: 30 mg twice weekly i.v./i.m.
• Branded Name: Bleocin, Oncobleo 15 mg inj.
Mitomycin:
• Use: In resistant cancer of stomach, cervix, colon, rectum,
bladder etc.
• Dose: 10 mg infused i.v. in one day.
• Branded name: Mytomycin C-2 10 mg inj.
Miscellaneous Cytotoxic Drugs
Hydroxyurea
Inhibit ribonucleotide reductase
Clinical uses: chronic granulocytic leukemia
Toxicity: bone marrow depression, nausea, vomiting
Dose: 20-30 mg/kg daily or 80 ml i.v. inj.
Branded Name: Cytodrox 500 mg cap.
Procarbazine:
Inhibit nucleic acid synthesis & cause chromosomal
damage.
Use : Oat cell carcinoma of lung.
Dose: 100-300 mg oral daily, maintenance dose 1-2
mg/kg/day
L- Aspar aginase
it inhibit the synthesis of L- Asparagines to L-aspartic acid
which cause the cell death.
AE: Liver damage, pancreatitis & CNS symptoms (due to
protein synthesis)
Dose: 50-200 KU/kg i.v. daily for 2-4 weeks
Cisplatin & Carboplatin
• Clinical uses:
– Genitourinary cancers, particular ovarian and bladder cancer
– Testicular cancer: in combination with Vinblastin and
Bleomycin
• Toxicity
– Acute toxicity: nausea, vomiting
– Renal toxicity: hydration with saline infusion & diuretics
– Myelosuppression
Dose: 50-100 mg every 3-4 weeks
Branded name: Cisplatin, cisplate, Plantinex 10 mg, 50 mg vial.
Dose: 400 mg i.v. infusion over 15-60 min.
Branded Name: Oncocarbin 150 mg inj, kemocrab 150, 450
mg/vial inj.
GnRH agonists
Hormones Indirectly inhibit the secretion of androgen
/estrogen by suppressing the FSH & LH
has effect on prostate/breast
Glucocorticoids
Primarily used in childhood acute
leukemia & lymphomas .
Secondary effect in Breast cancer Estrogens
Use in carcinoma of male breast.
120-240 mg orally.
Antiestrogen
Effective in positive estrogen receptor as
well as negative breast cancer in Anti Androgen
postmenopausal women. Palliative effect in advanced / metastatic
cases because it increase the androgen
level.
5 reductase inhibitor
Inhibit the conversion of testosterone to
dihydrotestosterone
Progestin
Use in temporary remission in some cases
of advanced & metastatic endometrial
carcinoma
Side Effects
•Toxic effects on normal cells
•Bone marrow suppression
•Bleeding
•Stomatitis
•Nausea, vomiting, diarrhea resulting in weight
loss, malnutrition
•Hair loss
•Fetal malformations
Toxicity of the
anticancer drugs
Acute toxicity
Common toxicity
• Myelosuppression
• Gastrointestinal disturbance
• Alopecia
Specific toxicity
• Cardiac toxicity: Daunorubicin
• Liver toxicity: CTX, Dactinomycin
• Bladder toxicity: CTX
• Neurotoxicity: VCR
• Hypersensitivity: Taxol
Chronic toxicity
• Infertility, teratogenesis, carcinogenesis
Three Possible Benefits of
Antineoplastic
• Cure
• Palliation—reduce or alleviate
symptoms, but do not eradicate
tumor
• Prolongation of life