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Flashcards in Biologic Drugs Deck (13)
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1
Q

Imatinib (MOA, Target, Heme-onc disease, resistance)

A

MOA: Tyrosine kinase inhibitor. Binds catalytic cleft of ABL on BCR-ABL fusion protein.

Target: ABL catalytic cleft

Disease: CML (t(9;22), Philadelphia chromosome, creates BCR-ABL fusion protein)

Resistance: ABL cleft mutates

2
Q

ATRA (MOA, Target, Heme-onc disease, toxicities)

A

MOA: Out-competes RAR-PML fusion protein to free RA receptor, allowing normal cellular differentiation

Target: RAR (retinoic acid receptor)

Disease: Acute Promyelocytic Leukemia (APML- AML subset)

Side effects:
-ATRA Syndrome: leukocytosis, capillary leak syndrome (pulmonary edema, respiratory failure), renal failure. Reduce with steroids/chemo

Resistance:

3
Q

Arsenic (MOA, Target, Heme-onc disease, toxicities)

A

MOA: Same thing as ATRA. Out-competes RAR-PML fusion protein to free RA receptor, allowing normal cellular differentiation

Target: RAR (retinoic acid receptor)

Disease: Acute Promyelocytic Leukemia (APML- AML subset)

4
Q

Rituximab (MOA, Target, Heme-onc disease)

A

MOA: Chimeric monoclonal antibody vs. CD-20, targeting pre/mature B-cell malignancies via immune activation

Target: CD-20

Disease: NHLs, autoimmune diseases

5
Q

Crizotinib (MOA, Target)

A

MOA: Tyrosine Kinase Inhibitor

Target: ALK, ROS1, HGFR

6
Q

Thalidomide ((MOA, Heme-onc disease, toxicities)

A

MOA: Teratogenic in fetus (dont grow arms), but mechanism really cutting off blood supply, good vs. cancer!

Target: unclear

Disease: MM, leprosy

Side effects: teratogenic

7
Q

Trastuzumab ((MOA, Target, Heme-onc disease, toxicities)

A

MOA: Binds HER-2 receptor, preventing dimerization and pathway oversignaling

Target: HER-2 receptor

Disease: Breast Cancer (20% HER-2+)

Side effects: Cardiac Toxicity

8
Q

Cetuximab (MOA, Target, Heme-onc disease, resistance)

A

MOA: chimeric monoclonal antibody to EGFR

Target: EGFR (human epidermal growth factor receptor)

Disease: NSCLC

Resistance: K-RAS and BRAF mutations

9
Q

Erlotinib (MOA, Target, disease)

A

MOA: Tyrosine kinase inhibitor

Target: EGFR (human epidermal growth factor receptor)

Disease: lung, breast, colon cancers

10
Q

Bevacizumab (MOA, Target, Heme-onc disease, toxicities, resistance)

A

MOA: Inhibits VEGF-R, inhibiting cancer angiogenesis

Target: VEGF-R

Disease:

Side effects:

  • hypertension
  • pulmonary hemorrhage
  • proteinuria
  • “financial toxicity”

Resistance:

11
Q

Vemurafinib (MOA, Target, Heme-onc disease, toxicities, resistance)

A

MOA: RAF inhibitor

Target: V600E BRAF mutation

Disease: NHL, hairy cell leukemia, melanoma, others

Side effects:
-Causes secondary skin cancers

Resistance: BRAF V600E mutations in colon cancer

12
Q

Bortezomib (MOA, Target, Heme-onc disease, toxicities)

A

MOA: Proteosome inhibitor- proteosome degradation is part of signaling pathway

Target: proteosome

Disease: Multiple myeloma

Side effects:

  • Neuropathy
  • myelosuppresion
13
Q

Nivolumab (MOA, Target, Heme-onc disease, toxicities, resistance)

A

MOA: tumors bind PD-1 receptor on T-cells inactivating them to prevent it targeting tumor. Nivolumab binds PD-1 receptor to block tumor deactivation of T-cells

Target: PD-1 receptor

Disease: HL, lots of other non-H/O

Side effects:

  • Immune-mediated pneumonitis, colitis, hepatitis, endocrinopathies
  • Fatigue
  • Rash/pruritis
  • Musculoskeletal pain

Resistance: