Drug Name Target Type Mode of Action Cancer

Cetuximab
Panitumumab
Sym004 EGFR Inhibits EGFR signaling by
MM-151 (ERBB1, Antibody binding to the extracellular
mAb 806 HER1) domain
mAb 528 Tumours overexpressing EGFR
MEHD7945A (lung and breast carcinoma for
Gefitinib example)
Erlotinib
EGFR Small molecule
Lapatinib Inhibits binding of ATP to the
(ERBB1, selective RTK
RTK ATP-binding pocket
Afatinib HER1) inhibitor
PD153035
AG1478
Trastuzumab Inhibits EGFR signaling by
ERBB2
Antibody binding to the extracellular Tumours overexpressing
Pertuzumab (HER2/neu)
domain HER2/neu (lung and breast
Lapatinib Small molecule carcinoma, HPV+ Head and
ERBB2 Inhibits binding of ATP to the
selective RTK neck carcinoma for example)
Afatinib (HER2/neu)
inhibitor
RTK ATP-binding pocket

Gleevec Incorporation into the

Small molecule CML cases with Philadelphia
BCR-ABL Tyrosine Kinase site of BCR-
(Imatinib) kinase inhibitor
ALB specifically
chromosome (95%)
HBS3 (Hydrogen Bond Oligopeptide (αH
H-Ras Inhibits Ras-SOS (GEF) Tumors with mutated Ras
Surrogate) helix of SOS)
interaction) function
DCAI/DCIE K-Ras Small molecule
SML-8-73-1
VSA9 K-Ras with Tumours with a K-Ras G12V
Small molecules Covalent locking of Ras-GDP
SML-10-70-1 G12V mutation (7% of lung cancers)
AA12
M2+ - cyclen
M2+ - BPA
Sulindac sulfide
Preventing Ras-Effector Tumors with mutated Ras
MCP110 Ras proteins Small molecules
interactions function
Kobe 0065
Kobe 2601
Kobe 2602
Torisel
Inhibition of mTOR activity
(Temsirolismus) mTOR “Small” molecule RCC and others
Afinitor (Everolimus)
Macugen (Pegapatanib) Nucleotide Strand - Inhibits VEGF 165 isomer -
VEGF 165 General antiangiogenic
aptamer antiangiogenic
Veglin VEGF- Prevents VEGFA/C/D
siRNA General antiangiogenic
A/C/D ecpression
Avastin CRC, nonsuamous non-SCLC,
Monoclonal Inhibition of VEGF signaling
VEGF-A metastatic breast cancer and
(Bevacizumab) Antibody by binding VEGF-A
RCC, recurrent Glioblastoma
Lucentis
(Ranibizumab)
Sutent (Sunitinib)
Nexavar (Sorafenib) Inhibition of VEGF-R RTK Metastatic and advance RCC,
Votrient (Pazopanib) VEGF-R Small RTK inhibitor
activity Breast cancer, CRC, and others
Recentin (Cediranib)
Axitinib
Vatalanib
XL184
Aflibercept Binding VEGFs in the ECM,
Chimeric soluble
(VEGF-Trap) All VEGFs
receptor
preventing VEGF/VEGF-R Metastatic CRC
(Regeneron) signaling
Bisphosphonates Prevents the activation of
“Bone Pyrophosphate-like Cancers that metastasize to the
enzymes which depends on
(BP) metabolism compound
pyrophosphate
bone

Atra (All-trans Retinoid All-trans retinoic Semms to induce cell

Leukemia
retinoic acid) receptors acid differentiation
Temozolomid Astrocytoma, Glioblastoma
DNA Small molecule DNA alkylating agent
(with inactivated GMT)
Olaparib Inhibits PARP function
causing SSBs to become Breast cancer with BRCA1/2
PARP Small molecule
DSBs (synthetic lethality in mutations
BRCA1/2 mutated cells)
Vinblastin Hodgkin’s lymphoa, NSCLC,
Small molecule Inhibition of microtubule
Tubulin melanoma, bladder, brain and
(vinca alkaloid) assembly – M phase arrst
testicular cancer
Carboplatin Ovarian, lung, head and neck
Pt-conjugated small
DNA DNA aquation (probably) and brain cancers,
molecule
neuroblastoma
Decitabine
Nucleotide Incorporate into DNA – bind
5-Azacytiine DNMT MDS/AML
analogues and inhibit DNMTs
Zebularine
SAHA Cutaneous T-cell lymphoma
HDACs Small molecules Inhibition of HDACs
Panobinostat Multiple myeloma