Oncology preparations

Cyclophosphamide

A: Chemotherapy agents, Alkylating agents, nitrogen mustard analog

B: 1. Cancer cells, alkalation in DNA structure → crosslinks formed → Inhib of DNA and RNA synthesis, Cytotoxic effect 2. B lymphocytes, Immunosuppressive effect

C: Breat cancer, Autoimmune diseases, immunosuppression in transplantology

SE: nausea, vomiting, hemorrhagic cystitis (Mesna as drug against it)

Doxorubicin

anthracycline antibiotic

A: Chemotherapy agents, Antitumor antibiotics

B: Inhibition of topoisomerase II, Interaction between nucleotides, Broduction of free radicals → inhib. of DNA and RNA synthesis, May induce apoptosis, Cytotoxic, Cytostatic

C: Breast cancer, Acute lymphotic leukemia

SE: highly emerogenic drug, alopecia, cardiotoxicity

Fluorouracil (5-FU)

A: Chemotherapeutic agents, Antimetabolites / Pyrimidine analogs, 5-FU – uracil analogue

B: Inhibition of DNA and RNA synthesis. 1 Fluoro-deoxyuridine monophosphate (FdUMF) → Inhib. of thymidylate synthetase, inhib. of DNA synthesis 2. Fluorouridine triphosphate (FUTP) → RNA synthesis inhib. Cytostatic effect, cytotoxic effect

C: Colorectal cancer, Breast cancer

SE: stomatotoxicity, weal emetogenic drug

Leucovorin - calcium folinate

A: Pharmacology of antimetabolites, active form of folic acid

C: 1. folic acid rescue therapy with moderate to high doses of MTX 2. In combination with 5-FU → potentiates 5-FU activity

Fludarabine

A: Chemotherapeutic agents, Antimetabolites / Purine analogs

B: DNA polymerase inhib., inhib. of ribonucleotide reductase, Inhib. of DNA synthesis → Cytostatic effec, cytotoxic effect

C: Chronic lymphocytic leukemia (CLL)

SE: Myelosuppression

Etoposide

A: Chemotherapeutic agents, Plant alkaloids, Topoisomerase II inhibitors

B: 1. Inhib. of Topoisomerase II 2. Free radicals production → DNA and RNA synthesis inhib. causes DNA double helix breaks, Inhib. mitochondrial function, can induce apoptosis → Cytotoxic, Cytostatic

C: Lung cancer, acute leukemia, non-Hodgkins lymphoma

SE: neurotoxicity

Irinotecan

A: Chemotherapeutic agents, Plant alkaloids, Topoisomerase I inhibitors

B: topoisomerase I inhibition, Inhib. of replication and transcription, DNA and

RNA synthesis inhib., can induce apoptosis, cytotoxic, cytostatic

C: Colorectal cancer

SE: diarrhea

!!: causes single strand DNA break, doesnt require ATP

Vincristine

A: Chemotherapeutic agents, Mitosis inhibitors

B: Inhib. of β-tubulin, inhib. microtubule polymerization → inhib. mitosis, cytotoxic, cytostatic

C: Leukemia

SE: neurotoxicity

!!: Resistance problem

Paclitaxel

A: Chemotherapeutic agents, Mitosis inhibitors

B: Inhibition of β-tubulin, inhibits microtubule depolymerization → inhib. mitosis, cytotoxic, cytostatic

C: Breast cancer, lung cancer (combination therapy with paclitaxel + doxorubicinn + cyclophosphamide)

SE: neurotoxicity, risk of tissue damage (necrosis) in case of extravasation

Imatinib

A: Targeted anticancer agents, Kinase inhibitors

B: Inhibition of Bcr-abl tyrosine kinase, prevents signaling protein

autophosphorylation, Cytostatic effect, Induces apoptosis only in Bcr-abl positive cells as well as in acute leukemia cells and acute lymphotic leukemia

C: Chronic myeloid leukemia (Philadelphia chromosome (bcr-abl) positive (Ph +)), Acute lymphocytic leukemia

Bevacizumab

A: Targeted anticancer agents, Inhibitors of angiogenesis

B: Anti-VEGF, inhibits the binding of VEGF to receptors on endothelial cells, Inhibits proliferation of vascular endothelial cells → reduces microvascularization of tumors, inhib. the formation of new tumorblood vessels. —→ Antiangiogenic activity, cytostatic

C: Metastatic colorectal cancer in combination with 5-FU, Diabetic maculopathy (macular edema) intravitreal

SE: Cardiotoxicity

Trastuzumab

A: Targeted anticancer agents, Growth factor inhibitors, Anti-EGF

B: Blocks HER2 domain, ANtibody defined cytotoxic effect, cytostatic effect

C: HER2 positive, metastatic breast cancer

SE: Cardiotoxicity

Rituximab

A: Targeted anticancer agents, Growth factor inhibitors, Anti-CD20

B: 1.Antibody-defined (antibody dependent) and complement-determined cytotoxic effects, Induces apoptosis 2. Immunosuppressive effect

C: Non-Hodgkins lymphoma, Rheumatoid arthritis

Pembrolizumab

A: Immunotherapy agents, Anti-PD-1

B: Blockade of the PD-1 receptor prevents its interaction with PD-L1 and PD-L2 ligands, Cytostatic, Induce apoptosis

C: Monotherapy for treatment of advanced or metastatic melanoma, In monotherapy or combination of various locally advanced metastatic tumors (head/neck cancer, bladder carcinoma, renal carcinoma)

SE: cardiotoxicity