Anticancer drugs Flashcards
1
Q
Bendamustine
A
Alkylating agent - Nitrogen mustard
Interfere with cellular replication by forming cross-linkages between DNA strands.
2
Q
Busulfan
A
Alkylating agent
Interfere with cellular replication by forming cross-linkages between DNA strands.
3
Q
Carmustine
A
Alkylating agent - Nitrosourea
Interfere with cellular replication by forming cross-linkages between DNA strands.
4
Q
Chlorambucil
A
Alkylating agent - Nitrogen mustard
Interfere with cellular replication by forming cross-linkages between DNA strands.
5
Q
Cyclophosphamide
A
Alkylating agent - Nitrogen mustard
Interfere with cellular replication by forming cross-linkages between DNA strands.
Immunosuppressant properties are considered to be due to cytotoxic effect on lymphocytes.
6
Q
Dacarbazine
A
Alkylating agent - Triazene
Interfere with cellular replication by forming cross-linkages between DNA strands.
7
Q
Ifosfamide
A
Alkylating agent - Nitrogen mustard
Interfere with cellular replication by forming cross-linkages between DNA strands.
8
Q
Melphalan
A
Alkylating agent - Nitrogen mustard
Interfere with cellular replication by forming cross-linkages between DNA strands.
9
Q
Procarbazine
A
Alkylating agent
Interfere with cellular replication by forming cross-linkages between DNA strands.
10
Q
Temozolomide
A
Alkylating agent - Triazene
Interfere with cellular replication by forming cross-linkages between DNA strands.
11
Q
Thiotepa
A
Alkylating agent
Interfere with cellular replication by forming cross-linkages between DNA strands.
12
Q
Daunorubicin
A
Anthracycline
Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines
13
Q
Doxorubicin
A
Anthracycline
Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines
14
Q
Epirubicin
A
Anthracycline
Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines
15
Q
Idarubicin
A
Anthracycline
Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines
16
Q
Mitozantrone
A
Anthracycline
Cell cycle nonspecific. Inhibit DNA and RNA synthesis by intercalation of DNA base pairs and prevent DNA repair by inhibiting topoisomerase II. Free radical production may also contribute to cytotoxicity. Mitozantrone, an anthracenedione, is structurally related to anthracyclines
17
Q
Brentuximab vedotin
A
Antibody-drug conjugate
Conjugate of an antibody (which binds to CD30 on tumour cells) and monomethyl auristatin E (MMAE), a microtubule disrupting agent that induces cell cycle arrest and apoptosis.
18
Q
Enfortumab vedotin
A
Antibody-drug conjugate
Conjugate of an antibody (which binds to nectin‑4 on tumour cells) and monomethyl auristatin E (a microtubule disrupting agent that induces cell cycle arrest and apoptosis).
19
Q
Gemtuzumab ozogamicin
A
Antibody-drug conjugate
Conjugate of an antibody (which binds to CD33 on tumour cells) and a cytotoxic agent (N‑acetyl-gamma-calicheamicin, which induces double-stranded DNA breaks and apoptosis).
20
Q
Inotuzumab ozogamicin
A
Antibody-drug conjugate
Conjugate of an antibody (which binds to CD22 on tumour cells) and a cytotoxic agent (N‑acetyl-gamma-calicheamicin, which induces double stranded DNA breaks and apoptosis).
21
Q
Sacituzumab govitecan
A
Antibody-drug conjugate
Conjugate of an antibody (which binds to Trop‑2 on tumour cells) and SN‑38 (a topoisomerase I inhibitor and the active metabolite of irinotecan).
22
Q
Trastuzumab deruxtecan
A
Antibody-drug conjugate
Conjugate of trastuzumab and deruxtecan (a topoisomerase I inhibitor). The actions of deruxtecan result in DNA damage and apoptosis and add to those of trastuzumab.
23
Q
Trastuzumab emtansine
A
Antibody-drug conjugate
Conjugate of trastuzumab and DM1 (a cytotoxic microtubule inhibitor). The actions of DM1 result in cell cycle arrest and apoptosis and add to those of trastuzumab.
24
Q
Alemtuzumab
A
Binds to CD52 antigen, which is found on the surface of most B and T lymphocytes, monocytes, macrophages and some granulocytes. Lysis of CD52-positive cells follows via a number of mechanisms.
25
Atezolizumab
Blocks the programmed death ligand 1 (PD‑L1) from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.
26
Avelumab
Binds programmed death ligand 1 (PD‑L1) and stops it from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.
27
Bevacizumab
Recombinant humanised monoclonal antibody; binds human vascular endothelial growth factor (VEGF) inhibiting formation of new blood vessels, reducing vascularisation and growth of tumours.
28
Blinatumomab
Recombinant bispecific antibody construct that binds to CD19 on B cells and CD3 on T cells, forming a link that results in the activation of T cells to eliminate CD19-positive B cells.
29
Cemiplimab
Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.
30
Cetuximab
Binds to the epidermal growth factor receptor (EGFR), thereby inhibiting proliferation and inducing apoptosis of tumour cells that over-express EGFR.
31
Daratumumab
Binds CD38 protein which is highly expressed on plasma cell clones in multiple myeloma and light chain amyloidosis, leading to cell death.
32
Durvalumab
Binds programmed death ligand 1 (PD‑L1) and stops it from binding to its receptors (PD‑1 and B7.1), reactivating cytotoxic T lymphocytes and the anti-tumour immune response.
33
Elotuzumab
Binds SLAMF7 protein which is highly expressed on multiple myeloma cells, leading to cell death.
34
Ipilimumab
Binds to the cytotoxic T lymphocyte-associated antigen 4 (CTLA‑4) resulting in an enhanced T cell mediated immune response which leads to tumour cell death.
35
Nivolumab
Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.
36
Obinutuzumab
Recombinant humanised monoclonal antibody that binds to CD20 on B lymphocytes resulting in cell lysis.
37
Panitumumab
Binds to the epidermal growth factor receptor (EGFR) resulting in inhibition of cell growth, induction of apoptosis and decreased production of inflammatory cytokines and vascular growth factor.
38
Pembrolizumab
Inhibits the programmed death 1 (PD‑1) receptor from binding to its ligands (PD‑L1 and PD‑L2) on tumour cells, reactivating cytotoxic T lymphocytes and anti-tumour immunity.
39
Pertuzumab
Recombinant humanised monoclonal antibody that binds to human epidermal growth factor receptor 2 (HER2) preventing its pairing with other members of the HER family. This arrests cell growth and induces apoptosis. Pertuzumab also activates an immune response that lyses tumour cells.
40
Rituximab
Binds to CD20 on B lymphocytes.
In cancer, it starts an immune response that lyses normal and malignant B cells. In chronic inflammatory diseases (eg rheumatoid arthritis), it suppresses immune response and inflammation by reducing T cell activation and resulting cytokine production.
41
Siltuximab
Binds to interleukin‑6 (IL‑6), inhibiting signalling pathways involved in B‑lymphocyte and plasma cell proliferation, and in inflammatory and immune responses.
42
Trastuzumab
Recombinant humanised monoclonal antibody that binds to human epidermal growth factor receptor 2 (HER2) and inhibits the proliferation of tumour cells that over-express HER2. Trastuzumab also activates an immune response that lyses tumour cells.
43
Azacitidine
Antimetabolite - Pyrimidine antagonist
Pyrimidine nucleoside analogue of cytidine. Appears to cause hypomethylation of DNA and have direct cytotoxic effects on abnormal haemopoietic cells in bone marrow.
44
Capecitabine
Antimetabolite - Pyrimidine antagonist
Converted to fluorouracil by a 3‑step process in which the final step is more active in malignant than normal cells.
45
Cladribine
Antimetabolite - Purine antagonist
Purine antimetabolite that inhibits DNA repair and synthesis, particularly in lymphocytes and monocytes.
46
Clofarabine
Antimetabolite - Purine antagonist
Purine antimetabolite that inhibits DNA repair and synthesis and induces apoptosis.
47
Cytarabine
Antimetabolite -Pyrimidine antagonist
Pyrimidine nucleoside analogue of cytidine. Cytarabine is converted intracellularly to a nucleotide that inhibits DNA synthesis.
48
Decitabine with cedazuridine
Antimetabolite - Pyrimidine antagonist
Decitabine is pyrimidine analogue that causes DNA hypomethylation leading to reactivation of tumour suppressor genes and apoptosis. Cedazuridine increases the oral bioavailability of decitabine (by inhibiting cytidine deaminase).
49
Fludarabine
Antimetabolite - Purine antagonist
Purine antimetabolite that inhibits DNA synthesis and induces apoptosis. Also reduces RNA and protein synthesis.
50
Fluorouracil
Antimetabolite - Pyrimidine antagonist
Pyrimidine antimetabolite which, following intracellular conversion to active metabolites, interferes with DNA and RNA synthesis.
51
Gemcitabine
Antimetabolite - Pyrimidine antagonist
Pyrimidine nucleoside analogue of cytidine. Gemcitabine is metabolised intracellularly to active nucleosides that inhibit DNA synthesis and induce apoptosis.
52
Hydroxycarbamide/ hydroxyurea
Antimetabolite
Inhibits DNA synthesis by interfering with the conversion of ribonucleotides to deoxyribonucleotides.
53
Mercaptopurine
Antimetabolite - Purine antagonist
Purine antimetabolite. Mercaptopurine is metabolised to thioguanine nucleotides which interfere with purine synthesis, impairing lymphocyte proliferation, cellular immunity and antibody responses. Cross-resistance with tioguanine occurs.
54
Methotrexate
Antimetabolite - Folic acid antagonist
Folic acid antagonist. Inhibits DNA synthesis and cell replication by competitively inhibiting the conversion of folic acid to folinic acid.
55
Pemetrexed
Antimetabolite - Folic acid antagonist
Inhibits key folate-dependent enzymes necessary for the synthesis of purine and thymidine nucleotides essential for cell replication.
56
Raltitrexed
Antimetabolite - Folic acid antagonist
Folate analogue that directly inhibits thymidylate synthetase. This interferes with thymidylic acid formation and in turn with the synthesis of DNA.
57
Tioguanine
Antimetabolite -Purine antagonist
Purine antimetabolite. Tioguanine is metabolised to thioguanine nucleotides which interfere with purine synthesis and formation of DNA and RNA. Cross-resistance with mercaptopurine occurs.
58
Trifluridine with tipiracil
Antimetabolite - Pyrimidine antagonist
Trifluridine is a thymidine analogue which interferes with DNA function in cancer cells, preventing their proliferation. Tipiracil increases the oral bioavailability of trifluridine (inhibits thymidine phosphorylase).
59
Apalutamide
Nonsteroidal Anti-androgens
Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.
60
Biclutamide
Nonsteroidal Anti-androgens
Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.
61
Darolutamide
Nonsteroidal Anti-androgens
Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.
62
Enzalutammide
Nonsteroidal Anti-androgens
Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.
63
Flutamide
Nonsteroidal Anti-androgens
Competitively inhibit the binding of androgen at androgen receptors. Nonsteroidal anti-androgens do not suppress androgen production and may even increase testosterone concentration.
64
Cyproterone
Steroidal Anti-androgen
Competitively inhibit the binding of androgen at androgen receptors. Cyproterone (a steroidal anti-androgen) also has progestogenic effects that result in decreased production of testosterone.
65
Anastrozole
Aromatase inhibitor
Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.
66
Exemestane
Aromatase inhibitor
Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.
67
Letrozole
Aromatase inhibitor
Aromatase enzymes (in fat, liver, muscle and breast tissue of postmenopausal women) convert circulating androstenedione and testosterone to estriol and estradiol. Aromatase inhibitors reduce tissue estrogen concentration.
68
Goserelin
Gonadotrophin-releasing hormone agonist
GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.
69
Leuprorelin
Gonadotrophin-releasing hormone agonist
GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.
70
Triptorelin
Gonadotrophin-releasing hormone agonist
GnRH initially stimulates synthesis of FSH and LH, transiently increasing serum testosterone in males or serum estrogen in females. Continuous administration of GnRH agonists inhibits gonadotrophin production, suppressing ovarian and testicular steroidogenesis and inhibiting the growth of certain hormone-dependent tumours.
71
Tamoxifen
Selective estrogen receptor modulator
Compete with estrogen for receptor sites in breast tissue (anti-estrogenic effect) inhibiting tumour growth. Also have estrogen agonist activity on endometrium, bone and lipids. Suppression of other growth factors and cytokines may occur.
72
Toremifene
Selective estrogen receptor modulator
Compete with estrogen for receptor sites in breast tissue (anti-estrogenic effect) inhibiting tumour growth. Also have estrogen agonist activity on endometrium, bone and lipids. Suppression of other growth factors and cytokines may occur.
73
Abiraterone
Inhibits CYP17, reducing androgen synthesis in testicular, adrenal and prostate tumour tissues.
74
Degarelix
GnRH antagonist
Inhibits gonadotrophin production, reducing testicular androgen synthesis.
75
Fulvestrant
Anti-estrogen
Competitively binds to estrogen receptors resulting in their down-regulation. Inhibits the growth of estrogen receptor-positive tumours.
76
Carboplatin
Platinum compound
Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.
Carboplatin causes more severe myelosuppression than cisplatin, with pronounced effects on platelets.
77
Cisplatin
Platinum compound
Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.
Cisplatin is more emetogenic, nephrotoxic and ototoxic, and causes more neuropathy (often irreversible) than carboplatin.
78
Oxaliplatin
Platinum compound
Platinum compounds are activated within the cell by displacement of chloride ions, leaving positively charged molecules that react with DNA. DNA replication, transcription and cell division are inhibited, ultimately inducing apoptosis. Other mechanisms may also be involved. Platinum compounds are cell cycle nonspecific.
79
Bortezomib
Proteasome inhibitor
Inhibit proteasomes (which degrade intracellular proteins including those involved in cell cycle control and growth), impairing cell growth which leads to apoptosis.
80
Carfilzomib
Proteasome inhibitor
Inhibit proteasomes (which degrade intracellular proteins including those involved in cell cycle control and growth), impairing cell growth which leads to apoptosis.
81
Cabazitaxel
Taxane
Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.
82
Docetaxel
Taxane
Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.
83
Paclitaxel
Taxane
Promote assembly of tubulin into stable non-functional microtubules, and inhibit disassembly, arresting cell cycles in late G2 and M phase.
84
Lenalidomide
Thalidomide analogue
Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.
85
Pomalidomide
Thalidomide analogue
Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.
86
Thalidomide
Thalidomide analogue
Thalidomide and its analogues, lenalidomide and pomalidomide, have multiple modes of action that are not fully understood and may vary depending on the disease. They include induction of apoptosis, anti-proliferative and anti-inflammatory effects, T cell stimulation, and reduced angiogenesis.
87
Irinotecan
Topoisomerase I inhibitor
Inhibit the enzyme topoisomerase I, thereby interfering with coiling and uncoiling of DNA during replication, which inhibits nucleic acid synthesis. Actions are specific for S‑phase.
88
Topotecan
Topoisomerase I inhibitor
Inhibit the enzyme topoisomerase I, thereby interfering with coiling and uncoiling of DNA during replication, which inhibits nucleic acid synthesis. Actions are specific for S‑phase.
89
Vinblastine
Vinca alkaloid
Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.
90
Vincristine
Vinca alkaloid
Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.
91
Vinorelbine
Vinca alkaloid
Bind to tubulin inhibiting its polymerisation and microtubule formation; results in mitotic arrest in metaphase. Cell cycle specific for M phase.
92
Anagrelide
Platelet production inhibitor
Selectively inhibits megakaryocyte maturation, reducing platelet concentration.
93
Arsenic trioxide
Not fully understood. Induces partial differentiation and promotes apoptosis of leukaemic cells and may also inhibit angiogenesis.
94
BCG / Mycobacterium bovis
Immunostimulant
BCG (bacillus Calmette-Guerin) is live, attenuated Mycobacterium bovis, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumour lesions of the bladder.
95
Bleomycin
Inhibits DNA and to a lesser extent RNA synthesis, produces single and double strand breaks in DNA possibly by free radical formation.
96
Dactinomycin
Complexes with DNA interfering with DNA-dependent RNA synthesis; also has immunosuppressant properties.
97
Eribulin
Binds to microtubules inhibiting their growth and induces formation of non-productive tubulin aggregates; arrests cell cycle in G2‑M phase.
98
Etoposide
Podophyllotoxin
Inhibits topoisomerase II resulting in DNA strand breaks and inhibition of cell division in the late S and G2 phases of the cell cycle.
99
Everolimus
mTOR inhibitor
Binds to the intracellular protein FKBP‑12. The protein–drug complex blocks the activity of mTOR kinase, inhibiting angiogenesis and tumour cell proliferation, growth and survival.
100
Mitomycin
Cell cycle nonspecific. Reduced to an active metabolite that cross links DNA, inhibiting its synthesis. At high concentrations, RNA and protein synthesis may also be inhibited.
101
Niraparib
Inhibits poly (ADP-ribose) polymerase (PARP) enzymes resulting in DNA damage and apoptosis.
102
Olaparib
Inhibits poly (ADP-ribose) polymerase (PARP) enzymes resulting in double-stranded DNA breaks. Tumour cells with mutated non-functional BRCA1 and 2 genes are unable to repair these DNA breaks, resulting in cell death.
103
Pegaspargase
Pegaspargase is the pegylated form of E. coli-derived asparaginase. Asparaginase is also known as L‑asparaginase or colaspase.
Asparaginase breaks down L‑asparagine; certain types of leukaemic cells cannot synthesise this essential amino acid and are therefore unable to grow and survive.
104
Romidepsin
Inhibits histone deacetylase (HDAC) resulting in altered gene expression, induction of cell differentiation, cell cycle arrest and apoptosis.
105
Selinexor
Inhibits the protein exportin 1, leading to reactivation of tumour-suppressing proteins and apoptosis in tumour cells.
106
Sonidegib
Binds to smoothened (SMO) transmembrane protein, inhibiting the hedgehog signalling pathway which is abnormally activated in some cancers.
107
Trabectedin
Interferes with the cell cycle by binding to DNA and altering its structure, affecting DNA binding proteins and repair pathways.
108
Tretinoin
Induces differentiation and inhibits cell proliferation in haemopoietic cell lines.
109
Venetoclax
Binds to and inhibits the B cell lymphoma 2 (BCL‑2) protein, which is an anti-apoptotic protein over-expressed in certain tumour cells, triggering cell death.
110
Vismodegib
Binds to smoothened (SMO) transmembrane protein, inhibiting the hedgehog signalling pathway which is abnormally activated in some cancers.
111
Vorinostat
Inhibits histone deacetylase (HDAC) leading to accumulation of acetylated proteins which induces cell cycle arrest, differentiation or apoptosis.
112
Filgrastim
G‑CSF
G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.
Pegfilgrastim and filgrastim appear to be clinically equivalent, although febrile neutropenia appears less common with pegfilgrastim.
113
Lipegfilgrastim
G‑CSF
G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.
Pegylated form of filgrastim; pegylation decreases their renal clearance and increases their half-life; clearance increases as neutrophil count increases. Limited data suggest that lipegfilgrastim is non-inferior to pegfilgrastim.
114
Pegfilgrastim
G‑CSF
G‑CSFs stimulate production and differentiation of neutrophils from blood precursor cells.
Pegylated form of filgrastim; pegylation decreases their renal clearance and increases their half-life; clearance increases as neutrophil count increases.
Pegfilgrastim and filgrastim appear to be clinically equivalent, although febrile neutropenia appears less common with pegfilgrastim.
115
Amifostine
Prodrug is activated to a free sulfhydryl (thiol) metabolite; its higher concentration in normal cells than cancer cells may explain the selective protection of normal cells from toxic effects of anticancer drugs and radiation.
116
Calcium folinate
Bypasses inhibition of dihydrofolate reductase by folic acid antagonists, eg methotrexate (folinic acid rescue) reducing their toxicity. Competes for cellular uptake with methotrexate.
Enhances the inhibition of thymidylate synthetase by fluorouracil, increasing its cytotoxicity.
117
Mesna
Contains free sulfhydryl (thiol) groups that interact with urotoxic metabolites, including acrolein, of ifosfamide and cyclophosphamide and reduce the incidence of haemorrhagic cystitis and haematuria. Enhances urinary excretion of cysteine, which may increase uroprotective effect.
118
Palifermin
Recombinant human keratinocyte growth factor
Binds to keratinocyte growth factor (KGF) receptor on epithelial cells increasing the rate of cell proliferation. KGF receptor has not been found on haemopoietic cancer cells.
119
Plerixafor
Reversible antagonist of the CXCR4 chemokine receptor, inhibiting the binding of CD34+ haemopoietic stem cells to marrow stroma, resulting in their mobilisation into the blood stream.
120
Rasburicase
Recombinant urate oxidase enzyme that catalyses the enzymatic oxidation of uric acid into allantoin, which is more water soluble than uric acid and less likely to precipitate in the renal tubules.
121
Abemaciclib
Kinase inhibitor
Inhibit cyclin-dependent kinases (CDK) 4 and 6
122
Acalabrutinib
Kinase inhibitor
Inhibit Bruton’s tyrosine kinase (BTK)
123
Afatinib
Kinase inhibitor
Inhibit epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), HER4
124
Alectinib
Kinase inhibitor
Inhibit anaplastic lymphoma kinase (ALK) receptor, rearranged during transfection (RET)
125
Asciminib
Kinase inhibitor
Inhibit BCR-ABL1
126
Axitinib
Kinase inhibitor
Inhibit vascular endothelial growth factor receptor (VEGFR) types 1–3
127
Binimetinib
Kinase inhibitor
Inhibit mitogen-activated extracellular kinases (MEK) 1 and 2
128
Brigatinib
Kinase inhibitor
Inhibit ALK receptor, ROS1
129
Cabozantinib
Kinase inhibitor
Inhibit hepatocyte growth factor receptor (HGFR, MET), VEGFR type 2, AXL
130
Ceritinib
Kinase inhibitor
Inhibit ALK receptor
131
Cobimetinib
Kinase inhibitor
Inhibit MEK1, MEK2
132
Crizotinib
Kinase inhibitor
Inhibit ALK receptor, MET, ROS1
133
Dabrafenib
Kinase inhibitor
Inhibit BRAF (including V600E and V600K)
134
Dasatinib
Kinase inhibitor
Inhibit BCR-ABL1, Src family, stem cell factor receptor (c‑Kit), ephrin receptor, platelet-derived growth factor receptor (PDGFR)
135
Encorafenib
Kinase inhibitor
Inhibit BRAF (including V600E and V600K)
136
Entrectinib
Kinase inhibitor
Inhibit ROS1, tropomyosin receptor kinases (TRK), ALK receptor
137
Erlotinib
Kinase inhibitor
Inhibit EGFR
138
Gefitinib
Kinase inhibitor
Inhibit EGFR
139
Gilteritinib
Kinase inhibitor
Inhibit FLT‑3
140
Ibrutinib
Kinase inhibitor
Inhibit BTK
141
Idelalisib
Kinase inhibitor
Inhibit phosphatidylinositol 3‑kinase
142
Imatinib
Kinase inhibitor
Inhibit BCR-ABL1, c‑Kit, PDGFR
143
Lapatinib
Kinase inhibitor
Inhibit EGFR, HER2
144
Larotrectinib
Kinase inhibitor
Inhibit TRK
145
Lenvatinib
Kinase inhibitor
Inhibit VEGFR types 1–3, fibroblast growth factor receptor (FGFR) types 1–4, PDGFR, c‑Kit, RET
146
Lorlatinib
Kinase inhibitor
Inhibit ALK receptor, ROS1
147
Midostaurin
Kinase inhibitor
Inhibit VEGFR type 2, PDGFR, c‑Kit, FLT‑3, protein kinase C
148
Nilotinib
Kinase inhibitor
Inhibit BCR-ABL1, c‑Kit, ephrin receptor, PDGFR
149
Nintedanib
Kinase inhibitor
Inhibit VEGFR types 1–3, PDGFR, FGFR types 1–3
150
Osimertinib
Kinase inhibitor
Inhibit EGFR (including T790M mutation)
151
Palbociclib
Kinase inhibitor
Inhibit CDK4, CDK6
152
Pazopanib
Kinase inhibitor
Inhibit VEGFR types 1–3, PDGFR, c‑Kit
153
Ponatinib
Kinase inhibitor
Inhibit BCR-ABL1, c‑Kit, FLT‑3, RET
154
Regorafenib
Kinase inhibitor
Inhibit VEGFR types 1–3, PDGFR, c‑Kit, RET; also inhibits Raf kinases
155
Ribociclib
Kinase inhibitor
Inhibit CDK4, CDK6
156
Ripretinib
Kinase inhibitor
Inhibit PDGFR, c‑Kit
157
Ruxolitinib
Kinase inhibitor
Inhibit JAK1, JAK2
158
Sorafenib
Kinase inhibitor
Inhibit VEGFR types 2–3, PDGFR, c‑Kit, FLT‑3; also inhibits Raf kinases
159
Sunitinib
Kinase inhibitor
Inhibit VEGFR types 1–3, PDGFR, c‑Kit, FLT‑3
160
Tepotinib
Kinase inhibitor
Inhibit MET
161
Trametinib
Kinase inhibitor
Inhibit MEK1, MEK2
162
Vandetanib
Kinase inhibitor
Inhibit VEGFR types 2–3, EGFR, RET
163
Vemurafenib
Kinase inhibitor
Inhibit
BRAF V600E and V600K
164
Zanubrutinib
Kinase inhibitor
Inhibit BTK
