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ONCOLOGY EXAM 1
| Drug | Class | Target | Indication | Major ADRs | Extra Notes |
|---|---|---|---|---|---|
| Gefitinib | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR | NSCLC pts with EGFR | increase in liver transamunases, intersitial lung disease | Good for non small cell lung cancer (NSCLC) - pts with specific mutations, Secondary resistance caused by mutations |
| Osimertinib | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR | Given to those who have T790M, mutation, exon 19 deletion or L868R mutations, making them non responsive to gefitinib | interstitial lung disease/pneumonitis/PE | IRREVERSIBLE EGFR inhibitor |
| Cetuximab | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR | Chimeric monoclonal antibody, need to evaluate KRAS mutation in colorectal cancer (makes RAS stay on) | BBW: infusion reactions and cardiopulmonary arrest, rash and diarrhea, development of rash = tumor repsonse | |
| Panitumumab | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR | Human monoclonal antibody for colorectal cancer. evaluate KRAS | BBW: dermatologic toxicities | |
| Lapatinib | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR, HER2 | to enhance efficacy of gefitinib | BBW: hepatotoxicity, avoid grapefuit (CYP3A4) | |
| Afatinib | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | EGFR, HER2, HER4 | NSCLC with EGFR mutation, can use if | P-gp substrate | IRREVERSIBLE |
| Tucatinib | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | HER2 | used with tratuzumab for HER2 breast cancer | Serious diarrhea and hepatotoxicity | highly selective for HER2, used with trastuzumab to target inside and ouside of cell |
| Trastuzumab | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | HER2 | Humanized antibody against HER2 (works on outside of cell), works in combo with tucatinib to attack. breast cancer | BBW: cardiomyopathy, infusion reaction, pulmonary tox, embro-fetal tox | Interaction with warfarin monitor INR |
| ado-trastuzumab emtansine | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | HER2 | trast linked to cytotoxin DM1, tras binds to HER2, is internalized and DM1 is released to stop cell cycle and cause apoptosis | BBW: hepatotoxicity, caridotoxicity, embryo-fetal toxicity | |
| fam-trastuzumab deruxtecan-nxki | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | HER2 | trast linked with DXd, DXd in released after internalization to causes DNA damage and apoptosis | BBW: intersititial lung disease and pneumonitis, embro-fetal toxixicty | |
| Pertuzumab | Tyrosine Kinase Inhibitor (Growth factor receptor antagonist) | HER2 | Humanized antibody targeting HER2, used with trastuzumab | BBW: left ventricular dysfunction, fetal toxicity | |
| Crizotinib | Tyrosine Kinase Inhibitor (Anaplastic lymphoma kinase inhibitors) | ALK, ROS1, MET | NSCLC and large cell lymphoma | serious lung disease/pneumonitis, hepatotoxicity, QT interval prolongation, bradycardia | interactions QT prolonging drugs, grapefruit/CYP3A4 inhibitors , often develops resistance |
| Alectinib | Tyrosine Kinase Inhibitor (Anaplastic lymphoma kinase inhibitors) | ALK, RET | ,2nd gen, better BBB penetraion than crizotinib | visual disturbances, photosensitivity, fetal harm | |
| Brigatinib | Tyrosine Kinase Inhibitor (Anaplastic lymphoma kinase inhibitors) | ALK, ROS1, FLT-3, EGFR variants | 2nd gen, better BBB penetraion than crizotinib | visual disturbances, photosensitivity, fetal harm | |
| Ensartinib | Tyrosine Kinase Inhibitor (Anaplastic lymphoma kinase inhibitors) | ALK, ROS1, EGFR | 2nd gen, better BBB penetraion than crizotinib | visual disturbances, photosensitivity, fetal harm | |
| Lorlatinib | Tyrosine Kinase Inhibitor (Anaplastic lymphoma kinase inhibitors) | ALK, ROS1 | third gen, efffective agiasnt ALK mutations, best option, can use after other drugs build resistance | hepatotoxicity, lung disease/pneumonitis, fetal harm | |
| Midostaurin | Tyrosine Kinase Inhibitor (FMS-like TK 3) | FLT3 | For acute myeloid leukemia (AML) Better for pts with TKD variant | CYP3A4 interactions | |
| Quizartinib | Tyrosine Kinase Inhibitor (FMS-like TK 3) | FLT3 | AML, better use for pts with ITD+ variant | BBW: QT prolongations, torsades de pointes, cardiac arrest, CI: hypokalemia, hypomagnesimia, long QT syndrome | CI: hypokalemia, hypomagnesemia, Long QT syndrome |
| Entrectinib | Tyrosine Kinase Inhibitor (tropomysin receptor kinase TRK) | TRK, ROS1, ALK | get ROS1 and ALK unlike larotrecitnib that only targets TRK abc | QT prolongation, heart failure CYP3A4 | |
| Larotrectinib | Tyrosine Kinase Inhibitor (tropomysin receptor kinase TRK) | TRK | Treatment of solid tumors | serious neurotoxicity and nephrotoxicity, CYP3A4 | |
| Repotrectinib | Tyrosine Kinase Inhibitor (tropomysin receptor kinase TRK) | TRK, ROS1 | second gen is more selective and targets ROS1 as well | serious neurotoxicity and hepatotoxicity, pneumonia CYP3A4 | |
| Pralsetinib | Rearranged During Transfection (transmembrane tkr) | RET | targets RET fusion + or RET mutant thyroid cancer | severe interstitial lung disease/pneumonitis and HTN, CYP3A4 | RET specific |
| Selpercatinib | Rearranged During Transfection (transmembrane tki) | RET, VEGFR, FGFR | targets RET fusion + or RET mutant thyroid cancer | hepatotoxicity requires monitoring every 2 weeks, HTJN requiring monitoring, QTc prolongation, impaired wond healing, CYP3A4, tumor lysis syndrome | |
| Amivantamab-vmjw | Mesenchymal epithelial transition (MET) kinase inhibitor (TKI) | MET, EGFR | targets EGFR exon 19, exon 21 L858R subs and exon 20 insertions | fetal harm, blood clots, PE, DVT, skin reactions, infusion. reactions | attacks EGFR and MET mutationshepatoctye growth factor |
| Capmatinib | Mesenchymal epithelial transition (MET) kinase inhibitor (TKI) | MET | targets NSCLC with mutation of MET exon 14 skipping | peripheral edema, dyspepsia, fatigue, CYP3A4 | hepatoctye growth factor |
| Tepotinib | Mesenchymal epithelial transition (MET) kinase inhibitor (TKI) | MET | targets NSCLC with mutation of MET exon 14 skipping | peripheral edema, dyspepsia, fatigue, musoskelatal pain, CYP3A4 | hepatoctye growth factor |
| Acalabrutinib | Brutons tyrosine kinase inhibitors (TKI) | BTK | made for flaws of first gen, prevent signaling fro B cell antigen receptors | acalabrutinib has less side effects than zanubrutinib, serious hemorrhaging, myelosuppression, DDIs with PPIS, antacids 3A4 | prevent b cell antigen receptor signaling |
| Zanubrutinib | Brutons tyrosine kinase inhibitors (TKI) | BTK | made for flaws of first gen, prevent signaling fro B cell antigen receptors | serious hemorrhaging, myelosuppression, DDIs with PPIS, antacids 3A4 | prevent b cell antigen receptor signaling |
| Asciminib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL | binds to the myristate pocket to keep ABL in the inactive state, targte al ADL mutants including T315I | ||
| Bosutinib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL | inhibits most imatinib resistant varient except T315I mutant | ||
| Dasatinib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL | binds to ATP site in ABL without regard to state of activation loop, so can be used for imatinib resistant genetic variants, some sarcoma kinase inhibition | ||
| Imatinib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL, PDGFR, KIT | for CML, GIST, CMML (chronic leukemia and GI stromal tumor) | neutropenia, thrombocytopenia | binds at ATP when activation loop is closed, inhibits platelet derived growth factor (PDGFR can cause angiogenesis) and KIT (CD117/stem cell factor) |
| Nilotinib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL | binds to ATP site in ABL wihtout regard to state of activation loop, so can be used for imatinib resistant genetic variants, has highest affinity for wild tyoe BCR-ABL | ||
| Ponatinib | Signal transduction antagonists, BCR-ABL antagonist | BCR-ABL | inhibits all imatinib resistant ABL including T315I | ||
| Dabrafenib | Signal transduction antagonists (B-RAF inhibitor) | B-RAF | melanoma, often used in combo with MEK inhibitor for better outcomes | QT prolongation, severe dermatologic reactions, photosensitivity | reactivation of MAPK pathway causes resistance |
| Encorafenib | Signal transduction antagonists (B-RAF inhibitor) | B-RAF | more BRAF coverage than dabrafenib for melanoma | QT prolongation, severe dermatologic reactions, photosensitivity, fetal risk, 3A4 | |
| Binimetinib | Signal transduction antagonists Mitogen-activated extracellular signal regulated protein kinase kinases + B-RAF) | MEK, BRAF | used for pts with BRAF V600E/K mutations | rare but serious rabdomylosis, retinal vein occlusion,. interstitial lung disease | |
| Trametinib | Signal transduction antagonists (Mitogen-activated extracellular signal regulated protein kinase kinases + B+RAF) | MEK, BRAF | used for multiple cancers with BRAF, inhibits MEK 1-2 | serious skin toxicity, cardiomyopathy, HTN, is ling disease, ocular toxic effects | secondary resistance built up do mutations in allosteric binding pocket at activation loop of MEK1, happens within -67 months |
| Abemaciclib | Cyclin dependent kinase inhibitors (CDK) | CDK | used in HR+ HER- breast cancer in combo with hormone therapy, prevent cells from replicating, inhibiting CDK 4 and 6 | serious pulmonary toxicity and blood clots, 3A4, GT interval elogating | take with food for increase absorption, abemaciclib thought to be most efficacious |
| Palbociclib | Cyclin dependent kinase inhibitors (CDK) | CDK | used in HR+ HER- breast cancer in combo with hormone therapy, prevent cells from replicating, inhibiting CDK 4 and 6 | serious pulmonary toxicity and blood clots, 3A4, GT interval elogating | take with food for increase absorption |
| Ribociclib | Cyclin dependent kinase inhibitors (CDK) | CDK | used in HR+ HER- breast cancer in combo with hormone therapy, prevent cells from replicating, inhibiting CDK 4 and 6 | serious pulmonary toxicity and blood clots, 3A4, GT interval elogating | take with food for increase absorption |
| Bevacizumab | Angiogenesis inhibitors | VEGF-A | used for renal cell carcinomas that overexpresss WEGF due to loss of VHL and HIF-1, can increase delivery of other chemotherapies, induces tumor hypoxia and starvation | increases risk of bleeding, proteinuria, hypertension | renal cell carcinomas nand used as adjuctive therapy in metastatic colon cancer |
| Thalidomide | Angiogenesis inhibitors | bFGF | multiple myeloma pts | teratogenic, thrombus, neuropathy | also works as an immunomodulator to enhance the immune system |
| Lenalidomide | Angiogenesis inhibitors | bFGF | second generation of thalidomide used for thalidomide refractory multiple myeloma | teratogenic, myelosuppression and thrombocytopenia, thrombus, neuropathy | also works as an immunomodulator to enhance the immune system |
| Atezolizumab | Immune checkpoint inhibitor | PD-L1 | various metastatic cancer with high PD-L1 expression | immune related effect (below), UTI, embryofetal toxicity | |
| Durvalumab | Immune checkpoint inhibitor | PD-L1 | advanced or metastatic urothelial carcinoma | upper respiratory infections, UTI, muscle pain, low appetite, SOB, rash | |
| Cemiplimab-rwlc | Immune checkpoint inhibitor | PD-1 | blocks PD-L1/2 (2nd ligand), used for treatmetn of advanced cutanous squamous cell carcinoma | monitor imine reactions, colitis, derm conditions, hepatitis, nephritis | |
| Nivolumab | Immune checkpoint inhibitor | PD-1 | metastatic melanoma approval in 2014 | uper respiratory tract infection, weakness, fever, rash, cough, nausea, back pain | |
| Pembrolizumab | Immune checkpoint inhibitor | PD-1 | used in metastatic NSCLC with over 50% PD-l! expression after platiunum based therapy, head and neck squamous cancer after platinum chemo | fatigue, rahs, pruritus, decreased appetite, dyspnea | long term response |
| Blinatumomab | Cell surface antigen monoclonal antibody | CD19/CD3 | CD3/19 antibody on malignant b cells and t cells, t cells link with tumor and trigger cell lysis, for treatment of b cell precursor | monitor for cytokine release syndrome, neurological toxicities and infections | |
| Obinutuzumab | Cell surface antigen monoclonal antibody | CD20 | humanized anti CD-20, improved receptor affinity causes programmed cell death (PCD) and antibody dependent cell mediated cytotoxicity (ADCC), for CLL and follicular lymphoma | infusionreactions, myelosuppression, HBV reactivation | |
| Rituximab | Cell surface antigen monoclonal antibody | CD20 | used in CD20 + NHL and CLL, effects normal mature b cells and cancerous b cells | immunosuppression due to targeting of normal ba cell, hypersensitivity due to chimeric nature. | |
| Venetoclax | BCL2 Inhibitor | BCL2 | allows apoptosis,m approved for CLL, small lymphocytic lymphoma and new AML in older adults | myelosuppression, upper respiratory tract infections, weekly dose escalation over first 5 weeks reduces the risk of tumor lysis syndrome | take oral formulation with food |
| Asparaginase | Asparaginase | Asparagine | acute lymph leukemia, decrease asparagine causes cell death | inhibition of nromal protein synthees, hypersensitivity in 5-20% of people , coma, pancreatitis | anitbiodies that can inactivage the enzyme may develop |
| Asparaginase erwinia chrysanthemi (recombinant)-rywn | Asparaginase | Asparagine | given second??? | normal cells can make ther own cancer needs to take it |
Created by:
beezy41