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Anticancer, Antimetabolites S-Phase, Adverse: Pancytopenia - Coggle…
Anticancer
Targeted Therapies
Growth Factor Inhibitors
MOA
Block cell growth and division enzymes
Drugs
Apoptosis-Inducing Drugs
MOA
Promote cell death
Angiogenesis Inhibitors
Inhibit growth of Blood vessels
Immune Checkpoint Inhibitorss
Block anti-T-Cell proteins
mTOR Inhibitors
MOA
Block mTOR (stop growth)
Hormonal Theraies
MOA
Prevents growth hormone binding to cancer cells
Natural Products
Mitotic Inhibitors (M-Phase)
Taxanes
MOA: Promote Microtubule Formation/
Prevents Microtubule Disassembly
Drugs (P D - Prevents Disassembly)
Paclitaxel
Docetaxel
Adverse
Bone Marrow Suppression
Fluid Retention (Docetaxel)
Vinca Alkaloids
MOA: Inhibits Microtubule Formation (Metaphase Arrest)
Restistance
Changes in Glycoprotein Transporter :red_flag:
Drugs
Vincristine
Indications
ALL
Wilms Tumor
Lymphoma
Vinblastine
Indications
Testicular Cancer
Hodgkins
Adverse
Neurotoxicity
SIADH
Topoisomerase Inhibitors
Topoisomerase I
MOA: Inhibit Topoisomerase I
Adverse
Myelosuppression
Delayed diarrhea + Cholinergic syndrome (Irinotecan)
Drugs
Topotecan
Indications
Ovarian
Small Cell Lung Cancer
Irinotecan
Combinations
Irinotecan + Leucovorin + 5FU
Colon Cancer
Topoisomerase II
MOA
Topoisomerase II inhibitor
Adverse
Myelosuppression
Secondary Leukemia (Etoposide)
Drugs
Etoposide
Indications
Testicular Cancer :red_flag:
Lung Cancer
Adverse
Alopecia
Teniposide
Indications
ALL :red_flag:
Antibiotics
Anticancer Antibiotics (Anthracyclines)
MOA
Intercalate
Inhibit Topoisomerase II
Generate Free Radicals
Inhibit DNA/RNA Synthesis
Alter Cell Membrane Fluidity
Adverse
Myelosuppression
Cardiomyopathy
Drugs
Doxorubicin (Adriamycin)
Indications
Breast Cancer
Adverse
Heart, arrhythmias, pericarditis
MOA
Intercalation
Daunorubicin
Indications
ALL
AML
Other Antibiotics
Bleomycin
MOA
Oxidative Damage/Free Radicals Leading to dsDNA Breaks
G2 Phase
Adverse
Pulmonary Fibrosis
Indications
Testicular Cancer
Hodgkin's
Dactinomycin (Actinomycin D)
MOA
Intercalates between Guanine-Cytosine :red_flag:
Inhibits DNA dependent RNA Pol.
Free Radical formation
Topoisomerase II inhibitor
Indications
Wilms Tumor
Adverse
Bone Marrow Depression
Proteasome Inhibitors
Drugs
Bortezomib
MOA
Blocks Proteasome-mediated degradation of IkB (preventing NF-kB) - 23S
Adverse
Peripheral Neuropathy
Indications
Multiple Myeloma
Drugs
Folate Antagonist
Methotrexate (MTX)
MOA
Converted to MTX-PG which inhibits Dihydrofolate Reductase
Resistance
Changes in glycoprotein transporter :red_flag:
Inhibition of regeneration of tetrahydrofolate (THF)
Indirectly inhibits thymidylate synthesis (Inhibition of DNA Synthesis) :red_flag:
Adverse
Bone Marrow Suppression
Hepatoxicity :red_flag:
Pulmonary Toxicity :red_flag:
Antidote (Tox reduce)
Leucovorine Rescue
Folinic Acid (Leucovorine) administered with MTX
Purine Antagonist
Azathioprine
6-Mercaptopurine (6-MP)
MOA
Activated by HGPRT
Inhibits PPRP
Metabolized (inactivated by TPMT) - reduces toxicity
Resistance
Tumor decreases activity of HGPRTase
Increase production of alkaline Phos. --> inactivates toxic nucleotides
Anditote
Xanthine Oxidase
6-Thioguanine (6-TG)
MOA
Activated by HGPRT
Cladribine (adenosine analog)
MOA
inhibit ADA and RNR
Hairy Cell Leukemia
Pentostatin
Inhibit ADA and RNR
Hair Cell Leukemia
Pyrimidine Antagonists
5-Flurouracil (5-FU)
MOA: Prodrug of FdUMP which inhibits Thymidylate Synthase
Combinations
5-FU + Leucovorin: increase effectively :red_flag:
Adverse
Bone Marrow Suppression :red_flag:
Neurotoxicity
Capecitabine (5-FU Prodrug)
MOA
Prodrug of F-FU
Adverse
Hand-Foot Syndrome :red_flag:
Bone Marrow Suppression
:red_flag:
Cytarabine
Cytosine Analogue
MOA
Inhibits DNA Pol.
Adverse
Cerebellar Dysfunction (ataxia) :red_flag:
Indications
AML
CML
Alkylating Agents
Drugs
Nitrogen Mustards
Mechlorethamine
Adverse:
Bone Marrow Suppression
Melphalan
Chlorambucil
Cyclophosphamide
MOA:
Converted to Phosphoramide Mustard (active) and acrolein (toxic)
Adverse
Hemorrhagic Cystitis
Antidote to Acrolein: MESNA
Nitrosoureas
Carmustine
Adverse
Bone Marrow Suppression
Lomustine
Streptozocin
Platinum
Cisplatin
MOA
intrastrand/interstrand crosslinks (sim to alky agents
Adverse
Nephrotoxicity
Antidote: Amifostine (Reduces Nephrotox.
Severe Nausea
Neurotoxicity
Carboplatin
Adverse
Bone Marrow suppression
Less Nephrotoxic
Oxaliplatin
Adverse
Peripheral Neuropathy
Others
Procarbazine
Adverse
Disulfiram Reaction
Increased risk of AML
Dacarbazine
Adverse
Bone Marrow Suppresson
Carcinogenic
Temozolomide
Adverse
Bone Marrow Suppression
Busulfan
Adverse
Pulmonary Fibrosis
Antimetabolites S-Phase
Adverse: Pancytopenia