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1

Alkylating Agents Mechanism

Produce strong electrophiles throughcarbonium or ethyleneimonium ionintermediates, which covalently bond viaalkylation of nucleophilic moieties in DNA(mostly N7 position of guanine); Cell CycleNon-Specific (CCNS)

2

Alkylating Agents Important Side Effects

Bone marrow, mucosal toxicity,nausea and vomiting, toxic effectson reproductive systems,increased leukemia risk

3

Alkylating Agents Miscellaneous

Resistance may occur due to:decreased permeability or uptake;increased rates of catabolism;enhanced DNA repair; increasedglutathione production (inactivatesvia conjugation)

4

List 11 Alkylating Agents

Mechlorethamine (Mustargen)Cyclophosphamide (Cytoxan)Ifosfamide (Ifex)Carmustine (Gliadel)Lomustine (Ceenu)Dacarbazine (DTIC)Procarbazine (Matulane)Temozolomide (Temodar)Cisplatin (Platinol)Carboplatin (Paraplatin)Oxaliplatin (Eloxatin)

5

Mechlorethamine class

(Mustargen)Nitrogen mustard

6

Mechlorethamine mechanism

Alkylating agent; spontaneous conversion to active metabolites in body fluids orenzymatically converted in liver

7

Mechlorethamine Therapeutics

Hodgkin's disease, topically for treatment of cutaneous T-cell lymphoma

8

Mechlorethamine "Other" side effects

Severe nausea and vomiting,myelosuppression (leucopenia,thrombocytopenia)

9

Mechlorethamine Misc

Don't use much anymore due to sterility

10

Cyclophosphamide(Cytoxan)Class

Nitrogen mustard

11

Cyclophosphamide(Cytoxan)Mechanism

Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard

12

Cyclophosphamide(Cytoxan)Therapeutics

Most widely used alkylating agent (broad clinical spectrum); singly or incombination for ALL, CLL, non-Hodgkin's lymphoma, and breast, lung, and ovarian cancer

13

Cyclophosphamide(Cytoxan)Important Side Effects

Hemorrhagic cystitis (bladderirritation) due to acrolein (toxicdrug metabolite); adequatehydration and administration ofMESNA (2-mercaptoethanesulfonate) minimizes problem

14

Cyclophosphamide(Cytoxan)"Other" Side Effects

Nausea, vomiting,myelosuppression

15

Cyclophosphamide(Cytoxan)Miscellaneous

Relatively long plasma half-life (7-15 hrs); taken orally

16

Difference between Ifosfamide and Cyclophosphamide

TherapeuticsIfos is used for Sarcoma and testicular cancerCyclophosphamide is the most widely used

17

Carmustine (Gliadel)Lomustine (Ceenu)Class

Nitrosoureas

18

Carmustine (Gliadel)Lomustine (Ceenu)Mechanism

Alkylating agent

19

Carmustine (Gliadel)Lomustine (Ceenu)Therapeutics

Brain tumors (cross blood-brain barrier)

20

Carmustine (Gliadel)Lomustine (Ceenu)Imp Side Effects

Renal toxicity, pulmonary fibrosis

21

Carmustine (Gliadel)Lomustine (Ceenu)Other side effects

Profound myelosuppression,severe nausea and vomiting

22

Dacarbazine (DTIC)class

Triazenes

23

Dacarbazine (DTIC)Mechanism

Alkylating agent; prodrug activated by livercytochromes

24

Dacarbazine (DTIC)Therapeutics

Part of ABVD for Hodgkin's disease; also, malignant melanoma

25

Dacarbazine (DTIC)"Other" Side Effects

Nausea and vomiting,myelosuppression (neutropenia, thrombocytopenia), flu-likesymptoms (fever, fatigue)

26

Dacarbazine (DTIC)Miscellaneous

IV administration

27

Procarbazine(Matulane)class

Triazenes

28

Procarbazine(Matulane)Mechanism

Alkylating agent; forms free radicals

29

Procarbazine(Matulane)Therapeutics

Hodgkin's lymphoma

30

Procarbazine(Matulane)Important side effects

May cause leukemia

31

Temozolomide(Temodar)class

Triazenes

32

Temozolomide(Temodar)Mechanism

Alkylating agent; nonenzymatic conversionto methylhydrazine at physiologic pH

33

Temozolomide(Temodar)Therapeutics

Malignant gliomas

34

Temozolomide(Temodar)"Other" Side Effects

Nausea and vomiting,myelosuppression (neutropenia,thrombocytopenia), flu-likesymptoms (fever, fatigue)

35

Temozolomide(Temodar)Miscellaneous

Taken orally

36

Cisplatin (Platinol)class

Platinum analogs

37

Cisplatin (Platinol)Mechanism

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

38

Cisplatin (Platinol)Therapeutics

Testicular, ovarian, cervical, andbladder cancers; also useful intreatment of head and neck cancer,and lung carcinoma

39

Cisplatin (Platinol)Imp Side Effects

Nephrotoxicity, ototoxicity,peripheral motor and sensoryneuropathy at high doses

40

Cisplatin (Platinol)Other side effects

Severe nausea and vomiting,mild to moderatemyelosuppression

41

Carboplatin(Paraplatin)Class

Platinum analogs

42

Carboplatin(Paraplatin)Mechanism

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

43

Carboplatin(Paraplatin)Therapeutics

Ovarian cancer

44

Carboplatin(Paraplatin)Other side effects

Myelosuppression(thrombocytopenia)

45

Oxaliplatin (Eloxatin)class

Platinum analogs

46

Oxaliplatin (Eloxatin)Mechanism

Alkylating agents that do not formcarbonium ion intermediates or formallyalkylate DNA; covalently bind nucleophilicsites on DNA (e.g., guanine N7); convertedto active cytotoxic forms by reacting withwater to form (+)charged, hydratedintermediates that react with DNA guanine,forming inter- and intrastand cross-links

47

Oxaliplatin (Eloxatin)Therapeutics

Gastric and colorectal cancer

48

Oxaliplatin (Eloxatin)Imp Side effects

Peripheral sensory neuropathy(cold-induced)

49

Oxaliplatin (Eloxatin)Other side effects

Neutropenia

50

Antimetabolites in general

Structural analogs of folic acid or of thepurine/pyramidine bases found in DNA; actin S-phase (cell cycle specific)

51

Antimetabolites list

Methotrexate (Trexall)Pemetrexed (Alimta)5-Fluorouracil (5-FU, Carac)Cytarabine (AraC, Depocyt)Gemcitabine (dFdC, Gemzar)6-Mercaptopurine (Purinethol)

52

Methotrexate (Trexall) class

Folate analogs

53

Methotrexate (Trexall) mech

Inhibits dihydrofolate reductase (DHFR),which converts dietary folate totetrahydrofolate (THF) needed for thymidineand purine synthesis; given orally orintrathecally

54

Methotrexate (Trexall) Therapeutics

Childhood ALL and choriocarcinoma;combination therapy for Burkitt'slymphoma and carcinomas of breast,ovary, head and neck, and bladder;administered intrathecally formeningeal leukemia and meningealmetastases of tumors (can't crossBBB); high-dose for osteosarcoma

55

Methotrexate (Trexall) Imp Side effects

Renal toxicity (crystallization inurine at high doses), hepatotoxicity(long-term, fibrosis/cirrhosis),reproductive (defective oogenesisor spermatogenesis, abortion)

56

Methotrexate (Trexall) Other side effects

Bone marrow(myelosuppression,spontaneous hemorrhage); GItoxicity (oral ulceration,stomatitis)

57

Methotrexate (Trexall) Misc

Can use leucovorin to prevent toxiceffects of MTX, as healthy cells cantake it up a lot better than tumor cells

58

Pemetrexed (Alimta) class

Folate analogs

59

Pemetrexed (Alimta) Mech

Polyglutamate forms that inhibit THFdependentenzymes (e.g., DHFR, TS);metabolized to polyglutamate forms thatinhibit THF-dependent enzymes (e.g.,DHFR, thymidylate synthase (TS))

60

Pemetrexed (Alimta) Therapeutics

Colon cancer, mesothelioma, non-smallcell lung cancer, pancreatic cancer

61

5-Fluorouracil (5-FU, Carac) class

Pyramidine analogs

62

5-Fluorouracil (5-FU, Carac) Mech

5-FU is converted to active metabolites: 5-FdUMP inhibits TS; 5-FdUTP incorporatesinto RNA & interferes with RNA function;prodrug [capesitabine] ribosylated and phophosrylated into5-FdUMP

63

5-Fluorouracil (5-FU, Carac) Therapeutics

Combination therapy for breast,colorectal, gastric, head and neck,cervical and pancreatic cancer;topically for basal cell carcinoma

64

5-Fluorouracil (5-FU, Carac) Imp Side Effects

Hand-foot syndrome (erythema,sensitivity of palms and soles),cardiac toxicity (acute chest pains)

65

5-Fluorouracil (5-FU, Carac) Other side effects

Anorexia and nausea; mucosalulcerations, stomatitis, diarrhea;thrombocytopenia and anemia

66

5-Fluorouracil (5-FU, Carac) Misc

Leucovorin can potentiate effects of5-FU; must be given IV (GI toxicityand rapid degradation + metabolismin gut and liver)

67

Cytarabine (AraC, Depocyt) Class

Pyramidineanalogs

68

Cytarabine (AraC, Depocyt) Mech

Ara-C converted by deoxycytidine kinase toAra-CMP --> Ara-CTP; terminates DNAsynthesis as Ara-CTP

69

Cytarabine (AraC, Depocyt) Therapeutics

AML (most effective treatment), ALLand blast phase CML

70

Cytarabine (AraC, Depocyt) Other side effects

Severe myelosuppression(leucopenia, thrombocytopenia,anemia), GI tract toxicity(ulceration, stomatitis, diarrhea)

71

Gemcitabine (dFdC, Gemzar) class

Pyramidineanalogs

72

Gemcitabine (dFdC, Gemzar) Mech

Converted to active metabolites: dFdCDPinhibits ribonucleotide reductase (lowersdeoxyribonucleotide); dFdCTP incorporatesinto DNA, terminating DNA synthesis

73

Gemcitabine (dFdC, Gemzar) Therapeutics

Pancreatic cancer; effective againstnon-small cell lung cancer, ovarian,bladder, esophageal, and head andneck cancer

74

Gemcitabine (dFdC, Gemzar) Other side effects

Myelosuppression (leucopenia,thrombocytopenia, anemia), flulike

75

Gemcitabine (dFdC, Gemzar) Misc

More effective against solid tumorsthan cytarabine

76

6-Mercaptopurine (Purinethol) Class

Purine analogs(antimetabolites)

77

6-Mercaptopurine (Purinethol) Mech

Prodrug metabolized by hypoxanthineguaninephosphoribosyl transferase(HGPRT) to 6-thioinosinic acid (TIMP);TIMP inhibits first step of de novo purinebase synthesis and the formation of AMPand xanthinylic acid from inosinic acid,reducing purine levels. As well, TIMP isconverted to thio-guanine ribonucleotides,inhibiting DNA and RNA synthesis

78

6-Mercaptopurine (Purinethol) Therapeutics

Maintain remission in acute ALL

79

6-Mercaptopurine (Purinethol) Imp side effects

Hepatotoxicity in prolonged use

80

6-Mercaptopurine (Purinethol) Other side effects

Bone marrow suppression

81

6-Mercaptopurine (Purinethol) Misc

Drug interaction with allopurinol (forgout), which inhibits xanthineoxidase; decrease 6-MP dose toavoid drug accumulation andtoxicities

82

DNA Intercalating Agents General Mechanism

Bind DNA through intercalation betweenspecific bases, blocking DNA, RNA or bothsynthesis; cause DNA strands to break andinterfere with cell replication; CCNS

83

Dactinomycin (Actinomycin D, Cosmegen) Mech

Intercalates G-C base pairs of DNA,interfering with DNA-dependant RNApolymerase; also causes ssDNA breaks

84

Dactinomycin (Actinomycin D, Cosmegen) Therapeutics

Pediatric tumors (Wilms' tumor,rhabdomyosarcoma Ewing's sarcoma);choriocarcinoma in women

85

Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects

Hematopoietic suppression withpancytopenia

86

Dactinomycin (Actinomycin D, Cosmegen) Other side effects

Anorexia, nausea, vomiting

87

Daunorubicin (Cerubidine) Class

Anthracyclines

88

Daunorubicin (Cerubidine) Mech

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA

89

Daunorubicin (Cerubidine) Therapeutics

AML

90

Daunorubicin (Cerubidine) Imp Side effects

Irreversible dose-dependentcardiotoxicity; alopecia

91

Daunorubicin (Cerubidine) Other side effects

Myelosuppression(neutropenia), stomatitis, GIdisturbances

92

Daunorubicin (Cerubidine) Misc

Dexrazoxane is cardio-protective

93

Idarubicin (Idamycin) Class

Anthracyclines

94

Idarubicin (Idamycin) Mech

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA

95

Idarubicin (Idamycin) Therapeutics

AML

96

Idarubicin (Idamycin) Imp Side effects

Irreversible dose-dependentcardiotoxicity; alopecia

97

Idarubicin (Idamycin) Other side effects

Myelosuppression(neutropenia), stomatitis, GIdisturbances

98

Idarubicin (Idamycin) Misc

Dexrazoxane is cardio-protective

99

Doxorubicin (Adriamicin, Doxil) class

Anthracyclines

100

Doxorubicin (Adriamicin, Doxil) Mech

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA

101

Doxorubicin (Adriamicin, Doxil) Therapeutics

Sarcomas, breast and lung carcinomas,malignant lymphomas

102

Doxorubicin (Adriamicin, Doxil) Imp side effects

Irreversible dose-dependentcardiotoxicity; alopecia

103

Doxorubicin (Adriamicin, Doxil) Other side effects

Myelosuppression(neutropenia), stomatitis, GIdisturbances

104

Doxorubicin (Adriamicin, Doxil) Misc

Dexrazoxane can be used to preventcardiotoxic effects

105

Epirubicin (Ellence) Class

Anthracyclines

106

Epirubicin (Ellence) Mech

Intercalate between DNA base pairs anddonate electrons to O2 to form superoxide;superoxide reacts with itself to form H2O2 --> cleaved in the presence of Fe to form OHradical, which cleaves DNA

107

Epirubicin (Ellence) Therapeutics

Metastatic breast cancer, gastriccancer

108

Epirubicin (Ellence) Imp side effects

Irreversible dose-dependentcardiotoxicity; alopecia

109

Epirubicin (Ellence) Other side effects

Myelosuppression(neutropenia), stomatitis, GIdisturbances

110

Epirubicin (Ellence) Misc

Dexrazoxane can be used to preventcardiotoxic effects

111

Bleomycin (Blenoxane) Mech

Acts in G2 phase of cell cycle. Binds toDNA, producing ss- and dsDNA breaks

112

Bleomycin (Blenoxane) Therapeutics

Combination therapy for testiculartumors or Hodgkin's disease;squamous cell carcinomas andlymphomas

113

Bleomycin (Blenoxane) Imp side effects

Pulmonary toxicity (pulmonaryfibrosis); cutaneous toxicity(hyperpigmentation,hyperkeratosis, erythema);hyperthermia

114

Bleomycin (Blenoxane) Other side effects

Minimally myelo- andimmunosuppressive (often usedin combo therapy); headache,nausea, vomiting

115

Bleomycin (Blenoxane) Misc

Dexrazoxane can be used to preventcardiotoxic effects

116

Microtubule Inhibitors

Inhibit mitosis and cause metaphase arrestby interfering with microtubule function(tubulin (de)polymerization); CCS

117

Vinblastine (Velban) Class

Vinca alkaloids

118

Vinblastine (Velban) Mech

Block tubulin polymerization intomicrotubules

119

Vinblastine (Velban) Therapeutics

Metastatic testicular tumors (withbleomycin, cisplatin); component ofABVD used for Hodgkin's disease

120

Vinblastine (Velban) Other side effects

Myelosuppression, nausea,vomiting

121

Vincristine (Oncovin) Class

Vinca alkaloids

122

Vincristine (Oncovin) Mech

Block tubulin polymerization intomicrotubules

123

Vincristine (Oncovin) Therapeutics

Childhood ALL (with glucocorticoids);Hodgkin's and non-Hodgkin'slymphomas

124

Vincristine (Oncovin) Important side effects

Dose-limiting neurotoxicity(peripheral neuropathy)

125

Vincristine (Oncovin) Other side effects

Relatively low bone marrowtoxicity

126

Paclitaxel (Taxol, Abraxane) Class

Taxanes

127

Paclitaxel (Taxol, Abraxane) Mech

Block microtubule depolymerization intotubulin

128

Paclitaxel (Taxol, Abraxane) Therapeutics

Metastatic breast, ovarian, lung, andhead and neck cancers

129

Paclitaxel (Taxol, Abraxane) Imp side effects

Peripheral neuropathy

130

Paclitaxel (Taxol, Abraxane) other side effects

Neutropenia; hypersensitivityreactions

131

Docetaxel (Taxotere) class

Taxanes

132

Docetaxel (Taxotere) Mech

Block microtubule depolymerization intotubulin

133

Docetaxel (Taxotere) Therapeutics

Metastatic breast, ovarian, lung, andhead and neck cancers; hormonerefractory prostate cancer

134

Docetaxel (Taxotere) Important side effects

Peripheral neuropathy

135

Docetaxel (Taxotere) Other side effects

Neutropenia; hypersensitivityreactions

136

Etoposide (Etopophos) class

Epipodophyllotoxins

137

Etoposide (Etopophos) mechanism

Inhibits topoisomerase II

138

Etoposide (Etopophos) Therapeutics

Testicular carcinoma, lung cancer, andnon-Hodgkin's lymphoma

139

Etoposide (Etopophos) other side effects

Dose-limiting myelosuppression(neutropenia), oral mucositis

140

Teniposide (Vumon) Class

Epipodophyllotoxins

141

Teniposide (Vumon) Mechanism

Inhibits topoisomerase II

142

Teniposide (Vumon) Therapeutics

ALL

143

Teniposide (Vumon) Other side effects

Dose-limiting myelosuppression(neutropenia), oral mucositis

144

Irinotecan (Camptosar) Class

Camptothecinanalogs

145

Irinotecan (Camptosar) Mechanism

Inhibits topoisomerase I

146

Irinotecan (Camptosar) Therapeutics

Advanced colorectal cancer; lung,ovarian, cervical and brain tumors

147

Irinotecan (Camptosar) Other side effects

Severe neutropenia, severediarrhea

148

Topotecan (Hycamtin) Class

Camptothecinanalogs

149

Topotecan (Hycamtin) Mechanism

Inhibits topoisomerase I

150

Topotecan (Hycamtin) Therapeutics

Ovarian and small cell lung cancer

151

Topotecan (Hycamtin) Other side effects

Severe neutropenia, severediarrhea

152

Prednisone (Meticorten) Class

Glucocorticoids

153

Prednisone (Meticorten) Mechanism

Inhibit mitosis in lymphocytes

154

Prednisone (Meticorten) Therapeutics

ALL; combination for Hodgkin's, non-Hodkin's, multiple myeloma, and CLL

155

Dexamethasone (Decadron) Class

Glucocorticoids

156

Dexamethasone (Decadron) Mechanism

Inhibit mitosis in lymphocytes

157

Dexamethasone (Decadron) Therapeutics

Reduces edema in brain and spinalcord tumors with radiation therapy

158

Tamoxifen (Soltamox) Class

Selectiveestrogen-receptormodulators(SERMs)

159

Tamoxifen (Soltamox) Mechanism

Competes with estradiol for binding toestrogen receptor

160

Tamoxifen (Soltamox) Therapeutics

ER-positive breast cancer, or asadjuvant therapy following primarybreast tumor excision; prevention ofbreast cancer in high-risk patients

161

Tamoxifen (Soltamox) Important side effects

Hot flushes, hair loss; increasedrisk of endometrial cancer;increased risk of thromboembolicevents

162

Tamoxifen (Soltamox) Other side effects

Nausea and vomiting

163

Fulvestrant (Faslodex) Class

Selectiveestrogen-receptordownregulators(SERDs)

164

Fulvestrant (Faslodex) Mechanism

Binds with much higher affinity (>100-fold)to estrogen receptor than tamoxifen,inhibiting dimerization, increasingdegradation, and reducing overall ER levels

165

Fulvestrant (Faslodex) Therapeutics

Posmenopausal women with ERpositivemetastatic breast cancer

166

Aminoglutethamide (Cytadren) Class

Aromataseinhibitors

167

Aminoglutethamide (Cytadren) Mechanism

Inhibits function of aromatase

168

Aminoglutethamide (Cytadren) Therapeutics

Relatively weak, used against breastcancer

169

Aminoglutethamide (Cytadren) Imp side effects

Significant

170

Anastrozole (Arimidex) Class

Aromataseinhibitors

171

Anastrozole (Arimidex) Mechanism

Inhibits function of aromatase

172

Anastrozole (Arimidex) Therapeutics

First-line for ER-positive breast cancerin postmenopausal women

173

Letrozole (Femara) class

Aromataseinhibitors

174

Letrozole (Femara) Mechanism

Inhibits function of aromatase

175

Letrozole (Femara) Therapeutics

ER-positive breast cancer inpostmenopausal women

176

Exemestane (Aromasin) class

Aromataseinhibitors

177

Exemestane (Aromasin) Mechanism

Steroidal inhibitor of aromatase

178

Exemestane (Aromasin) Therapeutics

ER-positive breast cancer inpostmenopausal women

179

Leuprolide (Lupron) class

GnRH analogs

180

Leuprolide (Lupron) Mechanism

Binds GnRH receptor; inhibits release ofFSH & LH

181

Leuprolide (Lupron) Therapeutics

Androgen ablation therapy, along withAR blockers

182

Goserelin (Zoladex) Class

GnRH analogs

183

Goserelin (Zoladex) Mechanism

Binds GnRH receptor; inhibits release ofFSH & LH

184

Goserelin (Zoladex) Therapeutics

Androgen ablation therapy, along withAR blockers

185

Flutamide (Eulexin) Class

Nonsteroidalandrogen-receptorblockers

186

Flutamide (Eulexin) Mechanism

Competes with androgen for AR binding

187

Flutamide (Eulexin) Therapeutics

Androgen ablation therapy, along withGnRH analogs

188

Bicalutamide (Casodex) Class

Nonsteroidalandrogen-receptorblockers

189

Bicalutamide (Casodex) Mechanism

Competes with androgen for AR binding

190

Bicalutamide (Casodex) Therapeutics

Androgen ablation therapy, along withGnRH analogs

191

Imatinib (Gleevac) Class

Tyrosine Kinaseinhibitor

192

Imatinib (Gleevac) Mechanism

Inhibits Abl kinase by binding where ATPshould go; also inhibits PDGFR and c-kit;metabolized by cytochrome P450

193

Imatinib (Gleevac) Therapeutics

First line therapy for CML; also,gastrointestinal tumor (GIST)

194

Imatinib (Gleevac) Imp Side effects

Nausea and vomiting, fluidretention, muscle cramps,arthralgia

195

Imatinib (Gleevac) Other side effects

Myelosuppression

196

Imatinib (Gleevac) Misc

Oral (1/day)

197

Gefitinib (Iressa) Class

Tyrosine Kinaseinhibitor

198

Gefitinib (Iressa) Mechanism

Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase

199

Gefitinib (Iressa) Therapeutics

Non-small lung cancer

200

Erlotinib (Tarceva) Class

Tyrosine Kinaseinhibitor

201

Erlotinib (Tarceva) Mechanism

Inhibit epidermal growth factor receptor(EGFR) tyrosine kinase

202

Erlotinib (Tarceva) Therapeutics

Non-small lung cancer

203

Nilotinib (Tasigna) class

Tyrosine Kinaseinhibitor

204

Nilotinib (Tasigna) Mechanism

Inhibits Abl kinase

205

Nilotinib (Tasigna) Therapeutics

Imatinib-resistant CML

206

Nilotinib (Tasigna) Imp side effects

Myelosuppression

207

Nilotinib (Tasigna) other side effects

QT prolongation, hepatotoxicity,electrolyte abnormalities

208

Nilotinib (Tasigna) misc

Oral (2/day)

209

Dasatinib (Sprycel) class

Tyrosine Kinaseinhibitor

210

Dasatinib (Sprycel) mechanism

Inhibits Abl & Src kinases

211

Dasatinib (Sprycel) therapeutics

Imatinib-resistant CML

212

Dasatinib (Sprycel) Imp side effects

Myelosuppression, bleeding, fluidretention, pulmonary arterialhypertension

213

Dasatinib (Sprycel) other side effects

Diarrhea, nausea and vomiting,weakness, infections

214

Dasatinib (Sprycel) misc

Oral (1/day)

215

Rituximab (Rituxan) class

Monoclonalantibody

216

Rituximab (Rituxan) mechanism

CD20 B-cell antibody that can directlyactivate apoptosis, activate complement, oractivate cell-mediated cytotoxicity (e.g., Tcells, NK cells)

217

Rituximab (Rituxan) therapeutics

Non-Hodgkin's lymphomas

218

Rituximab (Rituxan) imp side effects

Infusion reactions, tumor lysissyndrome (TLS), severemucocutaneous reactions,progressive multifocalleukoencephalopathy (PML)

219

Rituximab (Rituxan) other side effects

Skin reactions, irregularheartbeat, muscle or joint pain

220

Rituximab (Rituxan) misc

Patients need careful monitoring

221

Trastuzumab (Herceptin) class

Monoclonalantibody

222

Trastuzumab (Herceptin) mechanism

Unknown HER2/neu (ErbB2) receptorantibody mechanism (enhanced receptorendocytosis or blocking homo- orheterodimerization)

223

Trastuzumab (Herceptin) therapeutics

HER2/neu-overexpressing metastaticbreast cancer

224

Trastuzumab (Herceptin) Imp side effects

Hypersentivity reaction; ventriculardysfunction

225

Trastuzumab (Herceptin) misc

Usually combined with taxanes;enhances doxorubicin cardiotoxicity

226

Cetuximab (Erbitux) class

Monoclonalantibody

227

Cetuximab (Erbitux) mechanism

EGFR1 (ErbB1)

228

Cetuximab (Erbitux) therapeutics

EGFR-positive metastatic colorectalcancer

229

Cetuximab (Erbitux) imp side effects

Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities

230

Cetuximab (Erbitux) other side effects

Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis

231

Cetuximab (Erbitux) misc

Clinical trials, probably combine withcisplatin

232

Cetuximab (Erbitux) class

Monoclonalantibody

233

Cetuximab (Erbitux) mechanism

EGFR1 (ErbB1)

234

Cetuximab (Erbitux) therapeutics

EGFR-positive metastatic colorectalcancer

235

Cetuximab (Erbitux) imp side effects

Allergic reactions, sudden cardiacdeath, dermatologic problems,infections, renal failure, electrolyteabnormalities

236

Cetuximab (Erbitux) other side effects

Asthenia/malaise, fever,nausea, constipation, interstitialpneumonitis

237

Cetuximab (Erbitux) misc

Clinical trials, probably combine withcisplatin

238

Ipilimumab (Yervoy) class

Humanmonoclonalantibody

239

Ipilimumab (Yervoy) mechanism

Cytotoxic T-Lymphocyte Antigen 4 inhibitor;stimulates immune system

240

Ipilimumab (Yervoy) therapeutics

Melanoma

241

Vemurafenib (Zelboraf) class

Serine/threoninekinase inhibitor

242

Vemurafenib (Zelboraf) mechanism

Inhibits oncogenic BRAF kinase

243

Vemurafenib (Zelboraf) therapeutics

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

244

Vemurafenib (Zelboraf) imp side effects

Arthralgia, fatigue, photosensitivity,nausea, alopecia, diarrhea, QTprolongation

245

Vemurafenib (Zelboraf) other side effects

Cutaneous squamous cellcarcinoma, keratoacanthoma,new primary cutaneousmelanoma

246

Vemurafenib (Zelboraf) misc

Superior to dacarbazine in Phase IIItrials

247

Dabrafenib (Tafinlar) class

Serine/threoninekinase inhibitor

248

Dabrafenib (Tafinlar) mechanism

Inhibits oncogenic BRAF kinase

249

Dabrafenib (Tafinlar) therapeutics

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

250

Dabrafenib (Tafinlar) imp side effects

Serious febrile drug reactions,uveitis and iritis, hyperglycemia,hyperkeratosis

251

Dabrafenib (Tafinlar) other side effects

Higher risk of developing above

252

Dabrafenib (Tafinlar) misc

May cause male infertility

253

Trametinib (Mekinist) mechanism

Inhibits MEK

254

Trametinib (Mekinist) therapeutics

Unresectable Stage III and IV ormetastatic melanomas w/BRAFmutations

255

Trametinib (Mekinist) imp side effects

Cardiomyopathy, retinal disorders,interstitial lung disease, seriousskin toxicities

256

Trametinib (Mekinist) other side effects

Rash, diarrhea, stomatitis,hypertension, pruritis

257

Trametinib (Mekinist) misc

May cause female infertility

258

Hydroxyurea (Hydrea) mechanism

Inhibits ribonucleoside diphosphatereductase

259

Hydroxyurea (Hydrea) therapeutics

CML (replaced by Imatinib),polycythemia vera, essentialthrombocythemia; treatment for sicklecell disease (increases Hb-F)

260

Retinoids Mechanism

ATRA induces terminal differentiation inmalignant immature promyelocytes, whichsubsequently apoptose

261

Retinoids Therapeutics

APL

262

Retinoids imp side effects

"Leukocyte Activation Syndrome"(LAS), an increase in WBCs (fever,weight gain, respiratory distress,serosal effusion, renal failure)

263

Retinoids misc

Combined w/anthracyclines;corticosteroids used to block "LAS"

264

Arsenic Trioxide (Trisenox) Therapeutics

Relapsed APL

265

Thalidomide (Thalomid) Therapeutics

Multiple myeloma and myelodysplasticsyndromes

266

Interferons

Hairy-cell leukemia, CML, and AIDSrelatedKaposi's sarcoma

267

ABVD

Doxorubicin (adriamycin), bleomycin,vinblastine, dacarbazine

268

CHOP

Cyclophosphamide, hydroxydoxorubicin,vincristine (oncovine), prednisone

269

MOPP

Mechlorethamine, vincristine (oncovine),procarbazine, prednisone

270

CMF

Cyclophosphamide, methotrexate, 5-fluorouracil

271

FEC

5-fluorouracil, epirubicin, cyclophosphamide

272

Class for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrol

Estradiol esters(steroidal)

273

Class for:Ethinyl estradiolMestranol

Alkyl estrogen

274

Mechanism for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

Absorbed through skin, mucus membranes,GI Tract; body-wide distribution via sexhormonebinding globulin

275

Therapeutics for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

Contraception, primary hypogonadism,postmenopausal hormone therapy

276

Imp side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

Weight gain, HTN; less commonly,may cause breast cancer, DVT,cervical and endometrial cancer

277

Other side effects for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

Nausea, breast tension/pain,vaginal bleeding, headache

278

Misc for:Estradiol (valerate & cypionate)Estrone sulfateEquilin sulfateQuinestrolEthinyl estradiolMestranol

Strongly contraindicated in breast orendometrial cancers, endometriosis,undiagnosed vaginal bleeds;relatively contradinicated inpregnancy, thromboembolic disease,HTN, hepatic disease, family historyof breast or uterine cancer

279

Diethylstilbestrol class

Non-steroidalsynthetic estrogen

280

Diethylstilbestrol Imp side effect

Increased risk of clear celladenocarcinoma of vagina & cervix

281

Tamoxifen citrate (Nolvadex) class

Non-steroidal antiestrogen;selectiveestrogen receptormodifier

282

Tamoxifen citrate (Nolvadex) mechanism

Blocks estrogen from binding ER andcausing growth in ER(+) breast cancer

283

Tamoxifen citrate (Nolvadex) therapeutics

ER(+) breast cancer

284

Tamoxifen citrate (Nolvadex) imp side effects

Pro-estrogenic effect on uterineepithelium (increase risk ofendometrial cancer); partialestrogen agonist in bone andendometrium

285

Tamoxifen citrate (Nolvadex) misc

Anti-estrogenic effect on mammaryepithelium; must be used in veryhigh doses

286

Clomiphene citrate (Clomid) class

Non-steroidal antiestrogen

287

Clomiphene citrate (Clomid) mechanism

Blocks estrogen binding to hypothalamicreceptors (no estradiol negative feedbackon gonadotropins) --> increased secretionof gonadotropins & LH --> ovulation

288

Clomiphene citrate (Clomid) therapeutics

Stimulate ovulation in patients whowant to get pregnant

289

Clomiphene citrate (Clomid) imp side effects

Hot flashes, multiple pregnancy

290

Clomiphene citrate (Clomid) other side effects

Stomach pain, headache, upsetstomach, vomit

291

Clomiphene citrate (Clomid) misc

Cis-isomer (zuclomiphene) is a weakestrogen agonist; trans-isomer(enclomiphene) is a potent estrogenantagonist

292

ClassMicronized progesteroneTransvaginal progesterone

Naturalprogesterone

293

Therapeutics forMicronized progesteroneTransvaginal progesterone

Contraception, hormone replacementtherapy

294

Imp side effects forMicronized progesteroneTransvaginal progesterone

Fatigue, drowsiness

295

Misc forMicronized progesteroneTransvaginal progesterone

Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)

296

Class for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

Syntheticprogesterone

297

Therapeutics for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

Contraception, hormone replacementtherapy

298

Imp side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

Edema, abdominal bloating; lesscommonly: strong androgeniceffects (hirsutism, acne)

299

Other side effects for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

Anxiety, irritability, depression,muscular pain; increased risk ofthrombus and PE

300

Misc for:MedroxyprogesteroneNorethindroneNorgestrelMegestrol

Contraindicated in thromboembolicdisorders or patients with such ahistory, liver disease (metabolised inthe liver), undiagnosed vaginalbleeding, pregnancy (atrophy ofendometrium leading to birthdefects)

301

Class for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

Combination pill

302

Mechanism for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

Constant level of estrogen suppresses FSH,LH surge; progesterone suppresses LHsurge, thickens cervical mucus, leads toendometrial atrophy

303

Therapeutics for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

Contraception

304

Imp side effects for:Monophasic Ortho-NovumBiphasic Ortho-NovumTriphasic Ortho-Novum

As with synthetic estrogen andprogesterones

305

Monophasic Ortho-Novum Misc

Consistent dose of estrogen andprogestin (only take 21 days)

306

Biphasic Ortho-Novum Misc

Fixed estrogen, progestin increasedfor days 11-21

307

Triphasic Ortho-Novum Misc

Fixed or variable estrogen, whileprogestin increases in 3 phases (1-7,8-14, 15-21)

308

Mini-pill class

Progestin only

309

Mini-pill mechanism

As progestin

310

Mini-pill Therapeutics

Less effective than combination pill forcontraception; use when patient hasestrogen contraindication; good inlactating women (estrogen reduces milkproduction)

311

Mini-pill imp side effect

More likely to produce irregularmenstrual cycle (estrogen requiredto provide stability to endometrium)

312

Mini-pill other side effect

Suppresses endometrial cancer

313

Levonorgestrel (Plan B) class

Syntheticprogestogen

314

Levonorgestrel (Plan B) Mechanism

Not known

315

Levonorgestrel (Plan B) Therapeutics

Prevent implantation

316

Levonorgestrel (Plan B) Imp side effect

Likely the same as combinationoral contraceptives

317

Levonorgestrel (Plan B) misc

Must be taken within 72 hours ofcoitus

318

Mifepristone (RU-486, Korlym) class

Anti-progestin;glucocorticoidreceptorantagonist

319

Mifepristone (RU-486, Korlym) Mechanism

Competitively binds to progesteronereceptor (leading to detachment of fetus);glucocorticoid recepter antagonist

320

Mifepristone (RU-486, Korlym) Therapeutics

Abortion; Cushing's Syndrome

321

Mifepristone (RU-486, Korlym) Misc

Must take early in pregnancy (by day49); oral administration; must begiven by doctor in medical facilityprepared for surgery if abortionincomplete

322

Class for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

PDE5 inhibitor

323

Mechanism for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

Bind catalytic site of PDE5; inhibits PDE5breakdown of cGMP --> decreased Ca -->smooth muscle relaxation --> erection

324

Therapeutics for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

Erectile dysfunction; does not trigger anautomatic erection, but improvesresponse to sexual stimulation

325

Imp side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

Headache, dizziness, change invision (NAION)

326

Other side effects for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)Tadalafil (Cialis)

Flushing, upset stomach, stuffyor runny nose, UTI, diarrhea

327

Misc for:Sildenafil citrate (Viagra)Vardenafil HCl (Levitra)

Oral (once/day max); half-life of 4hours, peak plasma concentration in1-2 hours; contraindicated if onnitrates or α-blockers (unsafe drop inBP)

328

Misc for:Tadalafil (Cialis)

Oral (once/day max); half-life of 17.5hours, peak plasma concentration in1-2 hours; contraindicate if onnitrates or α-blockers (unsafe drop inBP)