Antiangiogenesis Drugs--Fitz

Question 1

Bevacizumab

Answer 1

MOA: humanized monoclonal antibody against VEGF

TU: metastatic colorectal cancer w/ 5-FU, lung cancer, macular degeneration

Tox: GI performation*, wound dehiscence, hemoptysis, worsen coronary artery disease

Question 2

Sorafinib

Answer 2

MOA: VEGF and PDGF TK antagonists

TU: renal cell carcinoma

PK: CYP3A4 metabolism

Tox: CHF, MI, teratogenic, HTN, hemorrhage

Question 3

Pazopanib

Answer 3

MOA: VEGF and PDGF TK antagonist

TU: renal cell carcinoma

PK: CYP3A4 metabolism, high plasma protein binding, PO

Tox: CHF, MI, teratogenic, hepatotoxicity

Question 4

Sunitimib

Answer 4

MOA: VEGF and PDGF TK antagonist

TU: renal cell carcinoma

PK: CYP3A4 metabolism, high protein binding, PO

Tox: CHF, MI, teratogenic, hand-foot syndrome

Question 5

Everolimus

Answer 5

MOA: mTOR inhibition (anti-VEGF, G1/S transition block)

PK: CYP3A4 metabolism

Resistance: MDR

Tox: lymphoma, renal arterial and venous thrombosis

Question 6

Tamisorolimus

Answer 6

MOA: mTOR inhibition (anti-VEGF, G1/S transition block)

PK: CYP3A4 metabolism

Resistance: MDR

Tox: lymphoma, renal arterial and venous thrombosis

Question 7

Lenalidomide, pamalidomide, thalidomide

Answer 7

MOA: suppress immune and inflammatory response, antiangiogenic, Th2 > Th1 activation

TU: MM

PK: PO, renal excretion

Tox: peripheral neuropathy, DVT (warfarin indicated in MM), severe teratogenic effects (phocomelia)