Monoclonal Antibodies/TKIs

Question 1

What is the target for Alectinib, crizotinib? What are the SEs?

Answer 1

ALK

Edema, rash, and diarrhea

Tx for Non-small cell lung cancer

Question 2

What is the target for:
Erlotinib, gefitinib, afatinib

What are the SEs?

Answer 2

EGFR

SE: Rash, diarrhea
Tx: Non-small cell lung cancer

Question 3

What is the target for:
Imatinib, dasatinib, nilotinib

What are the SEs?

Answer 3

BCR-ABL (+other TKIs as well {eg c-KIT})

CML, ALL, GISTs

SE: myelosupression, incr. LFTs, edema, myalgias

Question 4

What is the target for:
Ruxolitinib

What are the SEs?

Answer 4

JAK1/2

Tx: Polycythemia Vera

SE: Bruises, incr. LFTs

Question 5

What is the target for:
Bortezomib, ixazomib, carfilzomib

What are the SEs?

Answer 5

Proteosome (induce arrest at G2-M phase via accumulation of abnormal proteins—> apoptosis)
Tx: multiple myeloma, mantle cell lymphoma
SE: peripheral neuropathy, herpes zoster reactivation (decr. T-cell activation—> decr. Cell-mediated immunity)

Question 6

What is the target for:
Vemurafenib, Encorafenib, Dabrafenib
What are the SEs?

Answer 6

BRAF

Tx: Melanoma (often co-admin w/MEK inhibitors (trametinib)

SE: Rash, fatigue, nausea, diarrhea

Question 7

What is the target for:
Palbociclib

What are the SEs?

Answer 7

Cyclin-dependent kinase (CDK) 4/6 (induces arrest at G1-S phase —> apoptosis)
TX: breast cancer
SE: myelosuppression, pneumonitis