Mechanism of Action

Chemotherapy

Anthracyclines: 💉

Intercalate into DNA, inhibit topoisomerase II, generate free radicals → DNA damage → cell death

• Doxorubicin (Adriamycin)

• Daunorubicin

• Epirubicin

• Idarubicin (Idamycin)

Topoisomerase inhibitors: 💉

Interfere with DNA unwinding and replication → cell death

Topoisomerase I inhibitors:

• Irinotecan

• Topotecan

Topoisomerase II inhibitors: 

• Doxorubicin (Adriamycin) (Anthracycline and Tomoisomerase II inh)

• Etoposide

Alkylating agents:

DNA cross-linking → inhibits replication → cell death

• Cyclophosphamide 💊 💉

• Ifosfamide 💉

• Busulfan 💉

• Melphalan 💊 💉

• Bendamustine 💉

• Carmustine 💉

• Lomustine 💊

• Temozolomide (Temodar) 💊

• Procarbazine 💊

• Dacarbazine 💉

Microtubule-targeting agents: 💉

Disrupt mitotic spindle formation → mitotic arrest → cell death

Taxanes: 

• Paclitaxel (Taxol)

• Docetaxel

• Cabazitaxel

Vinca alkaloids:

• Vincristine (Oncovin)

• Vinblastine

Platinum compounds: 💉

DNA cross-linking → inhibits replication → cell death

• Cisplatin

• Carboplatin

• Oxaliplatin

Antimetabolites: 

Hypomethylating agents (DNA hypomethylation→ reactivation of tumor suppressor gene):

• Acacitidine -SubQ

• Decitabine 💉

• Decitabine/cedazuridine (Inqovi) 💊

Antifolates:

• Methotrexate 💊 💉

• Pemetrexed (Alimta) 💉

• Raltitrexed 💉

Purine analogues:

• 6-mercaptopurine 💊

• 6-thioguanine 💊

• Fludarabine 💉

• Cladribine 💉

Pyrimidine analogues:

• Cytarabine 💉

• 5-fluorouracil (5-FU) 💉

• Gemcitabine (Gemzar) 💉

• Capecitabine (Xeloda) 💊

• Floxuridine 💉

Immunotherapy

PDL-1 inhibitors: 💉

• Atezolizumab

• Durvalumab (Imfinzi)

• Avelumab

PD-1 inhibitors: 💉

• Pembrolizumab (Keytruda)

• Nivolumab (Opdivo)

• Tislelizumab

• Cemiplimab

• Dostarlimab

• Retifanlimab

• Toripalimab

CTLA-4 inhibitors: 💉

• Ipilimumab

• Tremelimumab

Bispecific T-cell engager (BiTE): 💉

Binds two targets simultaneously (CD3 on T cells and Tumor-associated antigen on cancer cells) → directs T cells to the tumor → T-cell mediated cytotoxicity

• Blinatumomab

• Teclistamab

Immunomodulatory imide drugs (IMiDs): 💊

• Lenalidomide

• Thalidomide

• Pomalidomide

Targeted Therapy

BRAF inhibitors: 💊

• Vemurafenib

• Dabrafenib

• Encorafenib

• Sorafenib

• Regorafenib is technically a BRAF inhibitor, but it is not a clinically effective BRAF-targeted therapy (BRAF inhibitory activity is weak compared to selective BRAF inhibitors)

MEK inhibitors: 💊

(Often combined with BRAF inhibitors)

• Trametinib

• Cobimetinib

mTOR inhibitors:

• Sirolimus 💊

• Everolimus 💊

• Temsirolimus 💉

VEGF inhibitors: 💉

Monoclonal antibodies

Target the extracellular circulating ligand (VEGF protein) → preventing it from binding to its receptors → inhibit tumor angiogenesis → reduce tumor growth

• Bevacizumab (Avastin)

• Ramucirumab

• Aflibercept

  
  

VEGFR inhibitors:  💊

Small-molecule TKIs

Target the intracellular tyrosine kinase domain of VEGF receptors → blocking downstream signaling even after ligand binding → inhibit tumor angiogenesis → reduce tumor growth

• Sunitinib

• Sorafenib (VEGFR and BRAF inhibitor)

• Regorafenib

• Pazopanib

• Axitinib

• Cabozantinib

• Lenvatinib

• Fruquintinib

KRAS inhibitors:  💊

• Sotorasib

• Adagrasib

BCR-ABL inhibitors:  💊

• Imatinib

• Dasatinib

• Nilotinib

• Ponatinib

EGFR inhibitors:  💊

• Erlotinib

• Gefitinib

• Osimertinib (Tagrisso)

NTRK inhibitors: 💊

• Larotrectinib

• Entrectinib

• Repotrectinib

BTK inhibitors: 💊

• Ibrutinib

• Zanubrutinib

• Pirtobrutinib

• Remibrutinib

ROS1 inhibitors: 💊

• Entrectinib (NTRK and ROS1 inh)

• Repotrectinib (NTRK and ROS1 inh)

• Crizotinib (ALK and ROS1 inh)

• Lorlatinib (ALK and ROS1 inh)

ALK inhibitors:  💊

• Crizotinib

• Lorlatinib

• Alectinib

• Brigatinib

RET inhibitors: 💊

• Selpercatinib

• Pralsetinib

JAK-2 inhibitors: 💊

• Ruxolitinib

• Fedratinib

• Pacritinib

• Momelotinib

HER-2 inhibitors:

Tyrosine kinase inhibitor:  💊

• Lapatinib

• Neratinib

Monoclonal antibody: 💉

• Trastuzumab (Herceptin)

• Pertuzumab (Perjeta)

• Margetuximab

Antibody-drug conjugates: 💉

• Ado-trastuzumab emtansine

• Trastuzumab deruxtecan (Enhertu)

Proteasome inhibitors:

• Bortezomib (Velcade) 💉

• Carfilzomib 💉

• Ixazomib 💊

Phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitors: 💊

• Idelalisib

• Umbralisib

• Zandelisib

• Linperlisib

• Leniolisib

CD20 inhibitors: 💉

• Rituximab

• Ublituximab

• Obinutuzumab

• Ofatumumab

• Ocrelizumab

IDH inhibitor: 💊

IDH1 inhibitor:

• Ivosidenib

• Olutasidenib

IDH2 inhibitor:

• Enasidenib