Misc. Chemo Drugs

Question 1

Vemurafenib

Answer 1

Small Molecule, RAF inhibitor
- Targets V600E BRAF mutation
- BRAF mut– melanoma (50%), NHL, CRC, NSCLC, Papillary thyroid, Hairy cell leukemia
Toxcity:- causes other skin cancers
- BRAF inhibitor + MEK inhibitor prevents resistance mut.
- Addition of MEK inhibitor (tremetinib) prevents other skin cancers
- CRC w/ V600E mut. is resistant to vemurafenib

Question 2

Thalidomide

Answer 2

Tx for ereythema nodosum leprosum and has anti-cancer activity in MM (anti TNF alpha)

Question 3

ATRA

Answer 3

All Trans Retinoic Acid
- Acute PML tx– PML-RAR fusion protein causes acute differentiation and arrest of normal promyelocytes
- ATRA causes differentiation and apoptosis of APML cellso
ATRA Syndrome: Starts shortly after ATRA initiation
-Leukocytosis w/ high neutrophils
- Capillary leak syndrome (PE, resp failure)
- Renal Failure
Tx: Steroids, chemo, supportive Tx

Question 4

Arsenic

Answer 4

Targets PML-RAR in APML for degradation

Question 5

Bortezomib (Velcade)

Answer 5

Proteasome Inhibitor

• Standard part of MM tx, originally for cachexia
• Neuropathy, myelosuppression

Question 6

Rituximab (Rituxan)

Answer 6

Chimeric mAB against CD20

• Standard tx for B-Cell NHL
• Immune activation and CD20 function interference
• Also used as tx in autoimmune disease and other B-Cell malignancies

Question 7

Gentuzumab ogozomicin

Answer 7

• Humanized mAB to CD33 conjugated to the toxin calicheamicin
• CD33 expressed on myeloid precursors
• Tx for AML in the elderly
  Tox: - Siginificant BM suppression
• Increased incidence of vaso-occlusive disease on BMT

Question 8

Tamoxifen

Answer 8

Anti Estrogen

- Breast cancer treatment, esp. for early stage prophylaxis

Question 9

Ipilumamab

Answer 9

Anti CTLA4 Inhibitor

- Treatment for melanoma, single and in combo w/ nivolumab