Chapter 39
Antineoplastic Agents
Department of Pharmacology,
Yunyang Medical College
Lu Juan(卢娟)
Teaching outline
To master the categories of antineoplastic
drugs and the basic mechanisms.
To understand the principles of combination
of antineoplastic drugs , the pharmacologic
actions , clinical applications and adverse reactions .
Overview
Cancer incidence and treatment
measures
The development history of
cancer chemotherapy
Novel anticancer drug
the adaptation syndrome of antineoplastic drugs:
1.Systemic tumor
2.Some solid tumor which have good effect
to chemotherapy
3.the consolidation and adjuvant therapy as
post-operation and radiotherapy
4.the palliative treatment of Late, extensive
transfer and recurrent tumors
5.Neo-adjuvant chemotherapy
Five-year survival rate%
Before chemotherapy
Choriocarcinoma
Malignant mole
Acute leukemia
…
20
20
0
post chemotherapy
85~90
>90
50
眼科检查：双眼瞳孔区可见白色反光，双眼底可见肿瘤
Pharmacological Basis
GF (growth fraction)
composition of tumor cells :
Proliferating cell population
GF =
Whole-cell group
1、Proliferating cell population ---Targeting of
therapy
Rapidly growing tumors, the GF is greater , and
sensitive to drugs.
2、Group of non-proliferating cells
Including three parts of quiescent cells, no
proliferation cells (already differentiated cells) and
dead cells, in which quiescent cells are not sensitive
to drugs is a source of tumor recurrence.
Cell cycle, including：
Resting (G0 phase)
Proliferating cycle:
Presynthesis(G1 phase)
DNA synthesis(S phase)
Premitotic(G2 phase)
Mitosis(M phase)
G2
(19%)
S (39%)
no proliferation
cells
M(2%)
Dead cells
G1(40%)
(G0)
Proliferating cell population
sensitive to drugs.
Group of non-proliferating cells
a source of tumor recurrence.
一． the relationship between Cell proliferation cycle and
the anti-cancer drugs
Classification of antineoplastic agents
According to the role of cycles or phases
cell cycle specific agents, CCSA
cell cycle non-specific agents, CCNSA
G2
(19%)
S (39%)
no proliferation
cells
M(2%)
Dead cells
G1(40%)
(G0)
Proliferating cell population
sensitive to drugs.
Group of non-proliferating cells
a source of tumor recurrence.
二．The relationship between biochemistry and
antineoplastic agents
Classification of antineoplastic agents
According to the biochemical mechanism of action
Drugs that affecting nucleic acid biosynthesis
Drugs that damaging structure and function of DNA directly
Drugs that inhibiting synthesis of RNA by interfering with
transcription process
Drugs that affecting synthesis and functions of proteins
Drugs that affecting the balance of hormones
Other
Classification of antineoplastic agents
According to the chemical structure and source
Alkylating agents
Antimetabolites
antitumor antibiotics
plant alkaloids
Hormonal agents
三．Adverse reactions
（一）Recent toxicities一common toxicities

bone marrow depression——is the most
common serious adverse reactions

Gastrointestinal reactions

Hair follicle damage
（二）Recent toxicities一Specific toxicities
Renal toxicity and bladder toxicity
Pulmonary toxicity
Cardiotoxicity
Neurotoxicity
Ototoxicity
Immunosuppression
Hepatotoxicity
（三）Long-term toxicity
Infertility, mutagenic, teratogenic
carcinogenesis：Second primary tumor
Commonly used anti-cancer drugs
一．Alkylating agents （ cell cycle nonspecific agents ）
cyclophosphamide
二．Antimetabolites （ cell cycle specific
agents ）
methotrexate,MTX
三． antitumor antibiotics （ cell cycle
non-specific agents ）
ADM
四．plant alkaloids
vinblastine ,VLB
vincristine,VCR
长
春
花
Camptothecine
Podophyllotoxin
paclitaxel
五． Hormones
六．other
四．The principles of using drugs
长
春
花
Best Wishes for Your Success in Final Examination