New Drugs

Question 1

Imatinib (Gleevec)

Answer 1

Kinase Inhibitor

Acts as a BCR-Abl (Tyrosine kinase) inhibitor in CML and other Ph+ malignancies and gastric stromal tumors

Toxicities: GI, skin, myelosuppression, hepatic, CHF, hypertension

Small Molecule

Question 2

Gefitnib (Iressa) or Erlotinib

Answer 2

Kinase inhibitor

Acts as a EGFR-ERB1 (Tyrosine Kinase inhibitor) in non-small cell lung cancer and other tumors

Toxicities: Hepatotoxicity, pulmonary firbrosis

Question 3

Trastuzumab (Herceptin)

Answer 3

Monoclonal Antibody (to membrane receptor)

RhMab to transmembrane receptor EGFR subunit Her-2 overexpressed in some metastatic breast cancers and other tumors

Toxicities: infusion reactions, cardiotoxicity, CHF

Question 4

Pertuzumab (Perjeta)

Answer 4

Monoclonal Antibody (to membrane receptor)

RhMab preventing ERB2 homo- and heterodimerization

Toxicities: infusion reactions, cardiotoxicity

Question 5

Bevacizumab (Avastin)

Answer 5

Monoclonal Antibody (Angiogenesis inhibitor)

RhMab against the VEGFR, reducing vascularization of tumor, found useful in AMD, colorectal cancer, diabetic retinopathy, but withdrawn for breast cancer by FDA.

Toxicities: N,V,D,H, proteinuria, hypertension, thromboembolism

Question 6

Ipilimumab

Answer 6

Monoclonal Antibody (Checkpoint inhibitor)

Against CTLA4 which inhibits T-cell activation vs tumor

Used to treat melanoma

Toxicities: Immune mediated reactions, neuropathy, enterocolitis, hepatitis, dermatitis

Question 7

Lambrolizumab

Nivolumab

Answer 7

Monoclonal antibody-(checkpoint inhibitor)

Used to treat melanoma

Against PD-1 (Programmed cell death-1) which negatively regulated immune response to tumor

Toxicities: Immune mediated reactions, neuropathy, enterocolitis, hepatitis, dermatitis

Question 8

Endostatin

Answer 8

Endogenous protein that binds to integrins and tropomyosin

Inhibits metalloproteinases

Question 9

Bortezomib (Velcade)

Carfilzomib

Answer 9

Proteosome inhibitors (synthetic organic molecules that contain boron)

Inhibits the proteosome, disregulating metabolism of proteins controlling the cell cycle inducing UPR, ESR and apoptosis

Toxicities: Neurotoxicity

Question 10

Angiostatin

Answer 10

Endogenous plasminogen fragment keeping tumor cell metastasis quiescent

Question 11

Thalidomide

Lenalidomide

Pomalidomide

Answer 11

Inhibits bFGF and VEGF working as an angiogenesis inhibitor

Toxicities: neurotoxicity