Anti cancer drugs (part 3/3) - lipincott review for preparation of test and interview

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 STEROID HORMONE & ANTAGONIST


Removal of Hormone OR Treatment with Hormone to regress Tumor

Orcheictomy=removal of both testes in Prosthatic cancer

Prednisone

Synthhetic, Anti-inflammatory Corticosteroid…Cortisol at high dose,Lymphocytolytic, ↑uric acid due to breakdown of Lymphocytes

MOA inactive…reduced to Prednisolone by 11-β-hydroxysteroid dehydrogenase…

Bind to receptor & trigger production of Specific proteins

S.E ulcer, Pancreatitis, Hyperglycemia, Glaucoma, Osteoporosis,

Tamoxifen

 Estrogen antagonist…used in Estrogen-Positive Breast cancer… SERM (Selective Estrogen Receptor Modulator) weak Estrogenic activity

Toremifene

 used in Breast cancer in Postmenupausal women

MOA

Bind to Estrogen receptor.complex is nonfunctional…↓Estrogen…used with GnRH analog Leuprolide ↓Estrogen level

S.E

Thromboembolism,Vision blurred, Hypercalcemia, Vaginal bleeding,Hot flash

Aromatase inhibitors

Aromatase reaction=↑Estrogen synthesis from Androstenedione in liver,fat,skin,breast,muscle

Aminoglutethimide=Aromatase inhibitor…ϴPregnenolone synthesis from Cholesterol… ϴCortisone, ↑ACTH, Hydrocortisone used for prevention…

Anastrozole & Letrozole

nonsteroidal…Aromatase inhibitor….Sec-line therapy after Tamoxifen…more potent 96%...do not need supplementation of Hydrocortisone

Extemestane

Steroidal, Irreversible inhibitor of Aromatase…Acne,hair changes Progestins

Megestrol acetate

used in Metastatic Breast cancer & Endometrial neoplasm

Leuprolide & Goserelin

GnRH released by Hypothalamus…stimulate Anterior Pituitory to secrete Gonadotropin hormone LH,FSH…which stimulate Estrogen secretion…

MOA

analog of Gonadotropin…bind to receptor, Desensitize it…ϴ LH & FSH...Estrogen & Androgen release↓

Used in Prostatic cancer, Breast cancer…

S.E; Impotence, Tumor flare

Estrogen

 used in Prostatic cancer…ϴLH,↓Endrogen…

S.E; Thromboembolism,M.I,Stroke, Hypercalcemia, Gynecomastia, Impotence  

Flutamide,Nilutamide, Bicalutamide

Nonsteroidal,Antiandrogen….used in Prostate cancer… Bind to Androgen receptor…inhibit translocation…

Flutamide ϴ the inhibitory effect of Testosterone…↑LH,Testosterone…Combine with

Leuprolide…Cause hepatitis

 Nilutamide cause vision problem

MONOCLONAL ANTIBODIES

Used against single antigen type

Trastuzumab

Humanized onoclona antibody…used in HER2(Human Epidermalgrowth factor-Receptor protein-2) overexpressionn…also used in Breast cancer with Paclitaxel

MOA

antibody-dependent toxicity…↓VEGF(VascularEndothelial Growth Factor)

S.E

Back pain, Worsen CHF

Rituximab

1st Monoclonal approved for cancer…CD20 Antagonist…used in Post transplant Lymphoma…Fab of Rituximab bind to CD20 Antigen on B-Lmyphocyte…

ϴCD20 involved in cell differentiation & cellcycle…Complement & antibody dependent toxicity

S.E

Angioedema, Bronchospasm, Hypotension, Tumor Lysis syndrome(↑K,Ca,P,Uric)

Bavacizumab

Anti-angiogenesis agent…1st line in Colorectal cancer…Given with 5-FU

Cituximab

Chimeric Monoclonal…combined with Irinotecan

OTHER

Platinum Coordination Complex

Cisplatin

1st member of Platinum coordination comples…Emetogenic(severe vomit)…

Carboplatin used in Renal impair….G1,,S phase

MOA

Lose its Cl- in low Chloride milieu…bind to N7 of Guanine…form crosslinks, inhbit DNA,RNA synthesis

S.E=nephrotoxic,, ↓Mg,Ca,Ototoxiciity, Tinnitus,

Irninotecan& Topotecan

 “S”phase specific…Camptothecin analog…Lactone ring….

MOA

ϴTopoisomerase l…essential for DNA replication… SN-38active metabolite of Irinotecan By CarboxyEsterase, cleavage of Carbamate bond b/w Camptothecin & Dipiperidino

S.E

Neutropenia like Paclitoxel

Etoposid

Obtain from Alkaloid Podophyllotoxin…Block cell from S-G2phase…

ϴTopoisomerase ll…used in Oat Cell carcinoma of Lung…

Imatinib

used in GIT Stromal Tumor, Chronic Myeloid Leukemia…ϴTyrosine kinase

Geftininb

ϴEGFR (Epidermal Growth factor receptor)…used in non-small lung cancer

Procarbazine

Oxidation lead to Cytotoxic effects…ϴMOA…Disulfiram-like reaction on taking Alchol…Mutagenic,Embryotoxic

L-Asparginase

catalyzeDeamination of Asparginase→Aspartic acid+Ammonia…

deprive of Tumor cells from amino acids to support growth…

used to treat Childhood Acute Lymphocytic Leukemia with VX & Prednisone.

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