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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5282_Библиотеки_им_академика_М_И_Перельмана
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205
Anti-neoplastic
Agents
Vinblastine
Vinorelbine
(ii) Taxanes
Paclitaxel
Docetaxel
(f) Topoisomerase-2 Inhibitors
Etoposide
(g) Topoisomerase-1 Inhibitors
Topotecan
Irinitecan
(h) Antibiotics
Actinimycin-D
Doxorubicin
Daunorubicin
Bleomycin
Mitomycin-C
(i) Hormonal Therapy
(i) Aromatase inhibitors
Letrozole
(ii) 5-α-reductase inhibitors
Finasteride
Dutasteride
(iii) Antiandrogens
Flutamide
Bicalutamide
Common adverse effects of anticancer drugs
Anemia
206
A Textbook of Pharmaceutical
Chemistry
Tiredness
Nausea
Vomiting
Loss of appetite
Constipation
Alopecia (Hair loss)
Mechlorethamine
Structure:
N
C
l
C
l
Chemical name: 2-Chloro-N-(2-chloroethyl)-N-methylethan-1-amine.
Uses: It is useful in the treatment of prostate cancer. It is also used in the treatment of
Hodgkin’s disease and non-Hodgkin’s lymphoma.
Formulations: Tablet and Lotion.
Brand names: Mustargen and Mustine.
Cyclophosphamide
Structure:
O NH
P
N O
Cl
Cl
Chemical name: (RS)-N,N-bis(2-chloroethyl)-1,3,2-oxazaphosphinan-2-amine-2-oxide.
Uses: It is used in the treatment of cancer and autoimmune diseases.
Formulations: Tablet and Injectable.
Brand names: Endoxan and Cycloxan.
207
Anti-neoplastic
Agents
Busulfan
Structure:
O S
O
O
S
O
O
O
Chemical name: Butane-1,4-diyldimethanesulfonate.
Uses: It is useful in the treatment of chronic myelogenous leukemia and certain blood
disorders such as polycythemia vera (overproduction of red blood cells), myeloid metaplasia.
Formulations: Tablet and Injectable.
Brand names: Busuphan, Myleran and Busulfex IV.
Thiotepa
Structure:
P
N
S
N
N
Chemical name: 1,1’,1’’-Phosphorothioyltriaziridine.
Uses: In the treatment of breast cancer, ovarian cancer, Hodgkin’s, and non-Hodgkin’s
lymphomas. Used in the treatment of superficial tumors of the bladder.
To control the accumulation of fluid in the body cavities that may result from certain cancers.
Formulations: Tablet and Injectable.
Brand names: Thiotepa and Thioplex.
208
A Textbook of Pharmaceutical
Chemistry
Mercaptopurine
Structure:
N
H
N
H
N
N
S
Chemical name: 3,7-Dihydropurine-6-thione.
Uses: In the treatment of acute lymphatic leukemia.
Formulation: Tablet.
Brand names: Purinethol and Empurine.
Fluorouracil
Structure:
N
H
NH
O O
F
Chemical name: 5-Fluoro-1H,3H-pyrimidine-2,4-dione.
Uses: In the treatment of colon cancer, esophageal cancer, stomach cancer, pancreatic cancer,
breast cancer, and cervical cancer.
Formulations: Tablet and Injectable.
Brand name: Adrucil.
Cytarabine
Structure:
N
N
H
2
N
O
O
OH
OH
HO
209
Anti-neoplastic
Agents
Chemical name: 4-Amino-1-[(2R,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-
yl]-pyrimidin-2-one.
Uses: In the treatment of different forms of leukemia such as acute and chronic myelogenous
leukemia, acute lymphocytic leukemia.
Formulation: Injectable.
Brand names: Cytosar-U, Depocyt, Cytabin, and Remcyta.
Methotrexate
Structure:
N
N
N
NH
2
N
NH
2
N
H
3
C
HN
O
COOH
COOH
Chemical name: (2S)-2-[(4-{[(2,4-Diaminopteridin-6 yl)methyl](methyl)amino}benzoyl]-
pentanedioic acid.
Uses: It is useful in molar pregnancy as an abortifacient. (Molar pregnancy is an abnormal
form of pregnancy in which a non-viable fertilized egg implants in the uterus).
It is useful in the treatment of leukemia, lymphoma, lung, osteosarcoma, bladder, and
trophoblastic neoplasms.
It is used as a disease-modifying treatment for some autoimmune diseases, including
rheumatoid arthritis, psoriasis, psoriatic arthritis, Crohn’s disease.
Leucovorin (rescue agent) is a folic acid derivative. Methotrexate and the folic acid
antagonists block the body's production of folate. Leucovorin works by replacing folate in the
body and reducing the toxic effects of methotrexate.
Formulation: Injectable.
Brand names: Biotrexate and Neotrexate.
210
A Textbook of Pharmaceutical
Chemistry
Azathioprine
Structure:
N N
N
HN
S
N
N
N
O
O
Chemical name: 6-[1-Methyl-4-nitro-1H-imidazol-5-yl)sulfonyl]-7H-purine.
Uses: It is useful in the treatment of organ transplantation and to treat rheumatoid arthritis,
systemic lupus erythematosus, Behcet’s disease (Immune-mediated small-vessel systemic
vasculitis that often presents with mucous membrane ulceration and ocular problems).
It prevents kidney transplant rejection when used along with other medicines.
Formulation: Tablet.
Brand names: Imuran and Azoprine.
Cisplatin
Structure:
Pt
NH
3
Cl
NH
3
Cl
Chemical name: (SP-4-2)-Diaminedichloroplatinum.
Uses: In the treatment of advanced bladder cancer, metastatic ovarian cancer and metastatic
testicular cancer.
In the treatment of testicular, ovarian, bladder, head and neck, oesophageal, small and non-
small cell lung, breast, cervical, stomach and prostate cancer.
Formulation: Injectable.
Brand names: Cisplat, Platinol
®
and Platinol-AQ
®
211
Anti-neoplastic
Agents
Daunorubicin
Structure:
O
CH
3
O
O OH
OH
CH
3
O
OH
O O CH
3
OH
NH
2
Chemical name: (8S,10S)-8-Acetyl-10-[(2S,4S,5S,6S)-4-amino-5hydroxy-6methyl-oxan-2-
yl]-oxy-6,8,11-trihydroxy-1-methoxy-9,10-dihydro-7H-tetracene-5,12-dione.
Uses: In the treatment of acute myelogenous leukemia (AML), acute lymphoblastic leukemia
(ALL) and acute promyelocytic leukemia (APL).
Formulation: Injectable.
Brand names: Daunocin, Cerubidine
®
, and Daunomycin.
Doxorubicin
Structure:
O
H
3
C
O
O OH
OH
O
OH
O
O
NH
2
OH
OH
Chemical name: (7S,9S)-7-[(2R,4S,5S,6S)-4-Amino-5-hydroxy-6-methyloxan-2-yl]oxy-
6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione.
212
A Textbook of Pharmaceutical
Chemistry
Uses: It is useful in the treatment of acute myeloblastic leukemia, bone sarcoma, breast
cancer, endometrial cancer, gastric cancer, liver cancer, kidney cancer and neck cancer.
Formulation: Injectable.
Brand names: Adriamycin
®
and Rubex
®
.
Dactinomycin
It is useful in the treatment of Wilm’s tumor (Kidney cancer),
Ovarian (Germ cell) cancer.
Ewing’s sarcoma (Blue cell tumor found the bone or soft tissue).
Metastatic testicular tumor.
Soft tissue sarcoma.
Osteosarcoma.
Formulation: Injectable.
Brand names: Cosmegen
®
and Dacmozen.
Etoposide
It is useful in the treatment of testicular, bladder, prostate, lung, stomach, uterine, and
mycosis fungoides cancer.
It is also useful in the treatment of Hodgkin’s, non-Hodgkin’s lymphoma, and Kaposi’s
sarcoma (It causes patches of abnormal tissue to grow under the skin, in the lining of the mouth,
nose and throat).
It is also useful in the treatment of brain tumors and Ewing’s sarcoma.
Formulation: Injectable.
Brand names: Pelstasol, Toposar
®
, VePesid
®
, and Etopophos
®
.
Vinblastine
This drug is given to treat Hodgkin’s and Non-Hodgkin’s lymphoma, testicular, bladder,
prostate, lung, breast cancer.
Formulation: Injectable.
Brand names: Uniblastine, Cytoblastine, Alkaban-AQ
®
, and Velban
®
.
213
Anti-neoplastic
Agents
Vincristine
This drug is given to treat acute leukemia, Hodgkin’s, non-Hodgkin’s lymphoma, testicular,
bladder, prostate, lung, breast cancer.
It is also useful in the treatment of neuroblastoma, rhabdomyosarcoma, Ewing’s sarcoma,
Wilm’s tumor, multiple myeloma and thyroid cancer.
Formulation: Injectable.
Brand names: Mcocristine, Cytocristine and Oncovin
®
.
Mitotane
Structure:
C
l
ClCl
C
l
Chemical name: (RS)-1-Chloro-2-[2,2-dichloro-1-(4-chlorophenyl)-ethyl]-benzene.
Uses: It is useful in the treatment of adrenal cortical cancer that cannot be treated with
surgery. It reduces amount of natural steroids in the body.
Formulation: Injectable.
Brand name: Lysodren.
Drostanolone Propionate
Structure:
O
O
O
H
H H
H
214
A Textbook of Pharmaceutical
Chemistry
Chemical name: (2R,5S,8R,9S,10S,13S,14S,17S)-17-Hydroxy-2,10,13-trimethyl-
1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta-[a]-phenanthren-3-one.
Uses: It is an anabolic steroid and useful in the treatment of breast cancer.
Formulations: Tablet and Injectable.
Brand names: Masteron and Drolban.
Approved New Drugs
Opdivo (Nivolumab)
Mechanism of action: It binds to the PD-1 receptor and blocks its interaction with PD-L1
and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response, including the
anti-tumor immune response. It is used for the treatment of classical Hodgkin lymphoma.
Venclexta (Venetoclax)
Mechanism of action: It acts as an inhibitor of B-cell lymphoma 2 (BCL-2), an anti-
apoptotic protein. It is used for the treatment of chronic lymphocytic leukemia.
Cabometyx (Cabozantinib)
Mechanism of action: It acts by suppressing metastasis, angiogenesis, and oncogenesis by
inhibiting receptor tyrosine kinases and is used for the treatment of advanced renal cell carcinoma.
Lenvima (Lenvatinib)
Mechanism of action: It acts by multi receptor tyrosine kinase inhibitor that inhibits the
kinase activities of vascular endothelial growth factor. It is used for the treatment of advanced
renal cell carcinoma.
Keytruda (Pembrolizumab)
Mechanism of action: It binds to the PD-1 receptor, blocking both immune-suppressing
ligands, PD-L1 and PD-L2 from interacting with PD-1 to help restore T-cell response and
immune response. It is useful in the treatment of head, neck squamous cell cancer, cervical cancer,
and bladder cancer.
Lartruvo (Olaratumab)
Mechanism of action: It selectively binds the external domain of human platelet-derived
growth factor receptor (PDGFR)-α with high affinity and blocks ligand binding. It is useful in the
treatment of soft tissue sarcoma.
Rubraca (Rucaparib)
Mechanism of action: It is an inhibitor of PARP-1, PARP-2, and PARP-3 and additionally
decreases the formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell
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