anti-cancer drug identification

methotrexate (MTX)

• inhibitor of folate metabolism (inhibits DHFR)

Leucovorin (folinic acid)

• THF → MTHF

5-fluorouracil

• inhibitor of thymidylate synthase

Capecitabine

• inhibitor of thymidylate synthase

  • oral prodrug of 5-FU

6-Mercaptopurine (6-MP)

• inhibitor of purine metabolism (inhibits IMPDH)

Azathioprine

• inhibitor of purine metabolism (inhibits IMPDH)

  • prodrug for 6-MP

Thioguanine

• inhibitor of purine metabolism

  • (becomes an analog of GMP → DNA unstable → death)

Hydroxyurea

• inhibitor of ribonucleotide reductase

Cladribine

• purine (adenosine) analogue

Clofarabine

• purine (adenosine) analogues

Cytarabine

• pyrimidine (cytidine) analogues

Gemcitabine

• pyrimidine (cytidine) analogues

Vincristine

• Antimitotics

  • Vinca alkaloids

    • inhibit tubulin polymerization

Vinblastine

• Antimitotic

  • Vinca alkaloids

    • inhibit tubulin polymerization

Paclitaxel

• Antimitotics

  • Taxane

    • inhibit tubulin depolymerization

Docetaxel

• Antimitotics

  • Taxane

    • inhibit tubulin depolymerization

Nab-paclitaxel

• Antimitotics

  • Taxane

    • inhibit tubulin depolymerization

Abraxane

• Antimitotics (Nab-paclitaxel)

  • Taxane

    • inhibit tubulin depolymerization

Mechlorethamine

• alkylating agents (Nitrogen mustard)

  • add alkyl → guanine

Chlorambucil

• alkylating agents (Nitrogen mustard)

  • add alkyl → guanine

Melphalan

• alkylating agents (Nitrogen mustard)

  • add alkyl → guanine

Cyclophosphamide

• alkylating agents (Nitrogen mustard)

Bendamustine

• alkylating agents (Nitrogen mustard)

Cisplatin

• alkylating agent (platinum compound)

  • add platinum metal → DNA

Carboplatin

• alkylating agent (platinum compound)

  • add platinum metal → DNA

Oxaliplatin

• alkylating agent (platinum compound)

  • add platinum metal → DNA

Bleomycin

• alkylating agent (Natural compound)

  • chelates iron to form complex → ROS generation

irinotecan

• topoisomerase 1 inhibitor (prodrug)

SN-38

• topoisomerase 1 inhibitor (prodrug)

Etoposide

• topoisomerase 2 inhibitor

Mitoxantrone

• topoisomerase 2 inhibitor

Doxorubicin

• topoisomerase 2 inhibitor

• (+ iron-reactive → lipid peroxidation )

Daunorubicin

• topoisomerase 2 inhibitor

• (+ iron-reactive → lipid peroxidation )

dexrazoxane

• NOT ANTI-cancer drug

  • iron chelating agent used for cardio protective effects (used with doxorubicin)

Leuprolide

• continuous GnRH Agonist

Degarelix

• GnRH receptor antagonist

Dutasteride

• 5-alpha-reductase (type II) inhibitor

Bicalutamide

• androgen receptor antagonist

Enzalutamide

• androgen receptor antagonist

Abiraterone

• inhibitors of steroidogenesis (C17 inhibitor)

Anastrozole

• aromatase inhibitor

Letrozole

• aromatase inhibitor

Exemestane

• aromatase inhibitor

Fulvestrant

• selective estrogen downregulator (SERD)

Tamoxifen

• Selective estrogen receptor modulator (SERM)

Erlotinib

• EGFR inhibitor

Afatinib

• EGFR inhibitor

Lapatinib

• EGFR-HER2 dual inhibitor

Cetuximab

• EGFR inhibitor

Panitumumab

• EGFR inhibitor

Trastuzumab

• HER2 inhibitor

Pertuzumab

• HER2 inhibitor

Bevacizumab

• VEGF/VEGFR inhibitor

Sunitinib

• multi-kinase inhibitor

  • VEGFR + cKIT

Sorafenib

• multi-kinase inhibitor

Regorafenib

• multi-kinase inhibitor

Crizotinib

• EML4-ALK tyrosine kinase inhibitor

Ceritinib

• EML4-ALK tyrosine kinase inhibitor

Alectinib

• EML4-ALK tyrosine kinase inhibitor

Imatinib

• BCR-ABL inhibitor

Dasatinib

• BCR-ABL inhibitor

• multi-kinase inhibitor

Nilotinib

• BCR-ABL inhibitor

Bosutinib

• BCR-ABL inhibitor

Ponatinib

• BCR-ABL inhibitor

• multi-kinase inhibitor

Asciminib

• BCR-ABL inhibitor

ibrutinib

• Bruton’s tyrosine kinase inhibitor

acalabrutinib

• Bruton’s tyrosine kinase inhibitor

Zanubrutinib

• Bruton’s tyrosine kinase inhibitor

rituximab

• anti CD20 mABs

¹³¹I tositumomab

• anti CD20 mABs

Brentuximab

• antibody-drug conjugate

  • anti CD30 mAB conjugated with MMAE (antimitotic agent)

Nivolumab

• anti PD1 mAB

Pembrolizumab

• anti PD1 mAB