Oncology
171 drugs
ALK and ROS1 inhibitors
- About this sectionOral kinase inhibitors for lung cancers driven by an ALK or ROS1 gene fusion, found by testing the tumour.
- AlectinibALK receptor tyrosine kinase
- CrizotinibALK receptor tyrosine kinase (also ROS1 and MET)
- LorlatinibALK and ROS1 receptor tyrosine kinases
Alkylating agents
- About this sectionReactive drugs that bolt alkyl groups onto DNA, cross-linking its strands so a dividing cell can no longer…
- BendamustineDNA, cross-linked between strands
- BusulfanDNA (guanine N7), cross-linked by the alkyl sulfonate
- CarmustineDNA (guanine), alkylated and cross-linked; proteins carbamoylated
- ChlorambucilDNA (guanine N7), cross-linked by the mustard
- ChlormethineDNA (guanine N7), cross-linked by the mustard
- CyclophosphamideDNA (guanine N7), cross-linked by phosphoramide mustard
- DacarbazineDNA (guanine), methylated by MTIC
- IfosfamideDNA (guanine N7), cross-linked by ifosfamide mustard
- LomustineDNA and RNA, alkylated; proteins carbamoylated
- LurbinectedinDNA minor groove (guanines)
- MelphalanDNA (guanine N7), cross-linked by the mustard
- ProcarbazineDNA (methylated by activated procarbazine metabolites)
- StreptozocinDNA (guanine), methylated by the nitrosourea
- TemozolomideDNA (guanine O6 and N7), methylated by MTIC
- ThiotepaDNA (guanine N7), cross-linked by thiotepa and its active metabolite TEPA
Antiandrogens and androgen synthesis inhibitors
- About this sectionProstate cancer tablets that block the androgen receptor or stop the body from making androgens, usually…
- AbirateroneCYP17A1 (17α-hydroxylase/C17,20-lyase)
- ApalutamideAndrogen receptor (AR)
- BicalutamideAndrogen receptor (AR)
- DarolutamideAndrogen receptor (AR)
- EnzalutamideAndrogen receptor (AR)
- FlutamideAndrogen receptor (AR)
Antibody-drug conjugates (ADCs)
- About this sectionA monoclonal antibody carries a potent cytotoxic drug straight to cancer cells that display its target, such…
- Brentuximab vedotinCD30 (TNFRSF8) on lymphoma cells
- Enfortumab vedotinNectin-4, a cell adhesion protein on urothelial cancer cells
- Gemtuzumab ozogamicinCD33 (SIGLEC3) on myeloid leukaemia cells
- Inotuzumab ozogamicinCD22 on B-lymphoblasts
- Sacituzumab govitecanTROP-2 (TACSTD2), a surface protein of many epithelial cancers
- Trastuzumab deruxtecanHER2 (ErbB2) receptor on tumour cells
- Trastuzumab emtansineHER2 (ErbB2) receptor on tumour cells
Antimetabolites
- About this sectionLook-alikes of folate or DNA building blocks that jam the enzymes making nucleotides, so fast-dividing cells…
- AzacitidineDNA methyltransferase (DNMT1), trapped on DNA
- CapecitabineThymidylate synthase (inhibited by FdUMP made from fluorouracil)
- CladribineDNA synthesis and repair in lymphocytes (through cladribine nucleotides)
- CytarabineDNA polymerase (inhibited by ara-CTP, which is also built into DNA)
- DecitabineDNA methyltransferase 1 (DNMT1), trapped on DNA after the drug is built into it
- FludarabineDNA polymerase α, ribonucleotide reductase and DNA primase (inhibited by fludarabine triphosphate)
- FluorouracilThymidylate synthase
- GemcitabineRibonucleotide reductase (inhibited by gemcitabine diphosphate) and DNA synthesis
- HydroxycarbamideRibonucleotide reductase (its tyrosyl radical, in the M2 subunit)
- MercaptopurineDe novo purine synthesis and DNA/RNA, through thioguanine nucleotides
- MethotrexateDihydrofolate reductase (DHFR)
- PemetrexedThymidylate synthase (also DHFR and GARFT)
- TioguanineDNA/RNA and purine synthesis, through thioguanine nucleotides
- Trifluridine/tipiracilThymidine phosphorylase (blocked by tipiracil); DNA (trifluridine)
Antineoplastic monoclonal antibodies
- About this sectionIntravenous antibodies that bind one molecule on cancer cells or their blood supply (HER2, CD20, EGFR, VEGF)…
- AmivantamabEGFR and MET receptors (bispecific antibody)
- BevacizumabVascular endothelial growth factor A (VEGF-A)
- BlinatumomabCD19 on B cells and CD3 on T cells
- CetuximabEpidermal growth factor receptor (EGFR), extracellular domain III
- DaratumumabCD38, a surface glycoprotein abundant on myeloma plasma cells
- ObinutuzumabCD20 (B-lymphocyte surface antigen)
- PanitumumabEpidermal growth factor receptor (EGFR, HER1), extracellular domain III
- PertuzumabHER2 (ErbB2) receptor tyrosine kinase, extracellular dimerisation domain II
- RamucirumabVascular endothelial growth factor receptor 2 (VEGFR2, KDR) on endothelial cells
- RituximabCD20 (B-lymphocyte surface antigen)
- TrastuzumabHER2 (ErbB2) receptor tyrosine kinase, extracellular domain IV
Antitumour antibiotics
- About this sectionCancer drugs first found in Streptomyces bacteria: anthracyclines, bleomycin, dactinomycin and mitomycin…
- BleomycinDNA (oxidative strand cleavage)
- DactinomycinDNA (guanine–cytosine steps); blocks RNA polymerase
- DaunorubicinTopoisomerase IIα (and DNA, by intercalation)
- DoxorubicinTopoisomerase IIα (and DNA, by intercalation)
- EpirubicinTopoisomerase IIα (and DNA, by intercalation)
- IdarubicinTopoisomerase IIα (and DNA, by intercalation)
- MitomycinDNA (cross-links at guanine and adenine)
- MitoxantroneDNA topoisomerase II (and DNA, by intercalation)
Aromatase inhibitors
- About this sectionBreast cancer medicines that block aromatase, the enzyme that makes oestrogen from androgens in fat and…
- AnastrozoleAromatase (CYP19A1)
- ExemestaneAromatase (CYP19A1)
- LetrozoleAromatase (CYP19A1)
BCL-2 inhibitors (BH3 mimetics)
- About this sectionOral drugs that switch apoptosis back on in cancer cells that survive by overproducing BCL-2; venetoclax is…
- VenetoclaxBCL-2, anti-apoptotic protein of the mitochondrial membrane
Bispecific T-cell engagers
- About this sectionAntibodies with two arms: one grabs CD3 on the patient's T cells, the other a tumour antigen, so the T cell…
- TeclistamabBCMA (B-cell maturation antigen, TNFRSF17) on myeloma cells, and CD3 on T cells
BRAF and MEK inhibitors
- About this sectionOral drugs that block two steps of the MAPK pathway in BRAF V600-mutant melanoma, lung, thyroid and…
- BinimetinibMEK1 and MEK2 (MAP2K1/2) kinases
- DabrafenibBRAF serine/threonine kinase (V600E/K mutants)
- EncorafenibBRAF serine/threonine kinase (V600E mutant), also wild-type BRAF and CRAF
- TrametinibMEK1 and MEK2 (MAP2K1/2) kinases
BTK inhibitors
- About this sectionOral drugs that switch off Bruton tyrosine kinase, the hub of B-cell receptor signalling, in CLL and other…
- ZanubrutinibBruton tyrosine kinase (BTK)
CAR T-cell therapies
- About this sectionThe patient's own T cells, genetically engineered to recognise a tumour antigen such as CD19 or BCMA and…
- Axicabtagene ciloleucelCD19 on normal and malignant B cells
- TisagenlecleucelCD19 on normal and malignant B cells
CDK4/6 inhibitors
- About this sectionOral drugs that hold breast cancer cells in the G1 phase of the cell cycle; used with hormone therapy in…
- AbemaciclibCyclin-dependent kinases 4 and 6 (CDK4/6)
- PalbociclibCyclin-dependent kinases 4 and 6 (CDK4/6)
- RibociclibCyclin-dependent kinases 4 and 6 (CDK4/6)
Chemotherapy supportive agents
- About this sectionDrugs that protect healthy tissue from chemotherapy or its side products: the bladder, the heart, the kidney…
- AmifostineNormal tissue (thiol protection against cisplatin and radiation injury)
- Calcium folinateReduced-folate pool (bypasses dihydrofolate reductase)
- DexrazoxaneTopoisomerase II (catalytic inhibitor) and intracellular iron
- MesnaAcrolein and other urotoxic ifosfamide metabolites (in urine)
- RasburicaseUric acid (the drug is the enzyme urate oxidase)
FGFR inhibitors
- About this sectionOral kinase inhibitors for tumours driven by FGFR changes, such as bladder cancer and cholangiocarcinoma…
- ErdafitinibFibroblast growth factor receptor kinases (FGFR1–4)
- PemigatinibFibroblast growth factor receptor kinases (FGFR1–3)
FLT3 inhibitors
- About this sectionOral kinase inhibitors for acute myeloid leukaemia with FLT3 mutations: added to first-line chemotherapy or…
- GilteritinibFLT3 receptor tyrosine kinase (also other receptor tyrosine kinases)
- MidostaurinFLT3 receptor tyrosine kinase (also KIT and other kinases)
GnRH analogues (agonists and antagonists)
- About this sectionInjected peptides that switch off the pituitary signal to the testes or ovaries, lowering testosterone or…
- CetrorelixGonadotropin-releasing hormone receptor (GnRH-R) on pituitary gonadotroph cells
- DegarelixGonadotropin-releasing hormone receptor (GnRH-R)
- ElagolixGonadotropin-releasing hormone receptor (GnRH-R) on pituitary gonadotroph cells
- GanirelixGonadotropin-releasing hormone receptor (GnRH-R) on pituitary gonadotroph cells
- GoserelinGonadotropin-releasing hormone receptor (GnRH-R)
- LeuprorelinGonadotropin-releasing hormone receptor (GnRH-R)
- RelugolixGonadotropin-releasing hormone receptor (GnRH-R) on pituitary gonadotroph cells
- TriptorelinGonadotropin-releasing hormone receptor (GnRH-R)
Hedgehog pathway inhibitors
- About this sectionOral Smoothened blockers for advanced basal cell carcinoma and, with low-dose cytarabine, for AML. All cause…
- GlasdegibSmoothened (SMO) receptor
- SonidegibSmoothened (SMO) receptor
- VismodegibSmoothened (SMO) receptor
HER2 tyrosine kinase inhibitors
- About this sectionOral small molecules that block the HER2 kinase from inside the cell; used in HER2-positive breast cancer…
- LapatinibHER2 (ERBB2) and EGFR tyrosine kinases
- TucatinibHER2 (ERBB2) tyrosine kinase
Histone deacetylase (HDAC) inhibitors
- About this sectionEpigenetic drugs that block histone deacetylases, reopening silenced genes; vorinostat and romidepsin treat…
- RomidepsinHistone deacetylases (zinc-dependent enzymes)
- VorinostatHistone deacetylases (class I HDAC1, 2 and 3, and HDAC6)
Immune checkpoint inhibitors
- About this sectionAntibodies that release the brakes on T cells (PD-1, PD-L1, CTLA-4) so the immune system attacks the cancer…
- AtezolizumabProgrammed death-ligand 1 (PD-L1) on tumour and immune cells
- CemiplimabProgrammed cell death protein 1 (PD-1) on T cells
- DurvalumabProgrammed death-ligand 1 (PD-L1) on tumour and immune cells
- IpilimumabCytotoxic T-lymphocyte antigen 4 (CTLA-4)
- NivolumabProgrammed cell death protein 1 (PD-1) on T cells
- Nivolumab/relatlimabPD-1 (nivolumab) and LAG-3 (relatlimab) on T cells
- PembrolizumabProgrammed cell death protein 1 (PD-1) on T cells
Immunomodulatory imide drugs (IMiDs)
- About this sectionThalidomide and its relatives: «molecular glues» that make the cell's cereblon complex destroy proteins…
- LenalidomideCereblon (CRBN), substrate receptor of the CRL4 E3 ubiquitin ligase
- PomalidomideCereblon (CRBN), substrate receptor of the CRL4 E3 ubiquitin ligase
- ThalidomideCereblon (CRBN), substrate receptor of the CRL4 E3 ubiquitin ligase
Kinase inhibitors (targeted oncology)
- About this sectionOral cancer drugs that block a kinase the tumour depends on, such as BCR-ABL in CML or mutant EGFR in lung…
- AcalabrutinibBruton's tyrosine kinase (BTK)
- AfatinibEGFR tyrosine kinase domain
- AsciminibBCR-ABL1 tyrosine kinase (myristoyl pocket of ABL1)
- BosutinibBCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases
- DasatinibBCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases
- ErlotinibEGFR tyrosine kinase domain
- GefitinibEGFR tyrosine kinase domain
- IbrutinibBruton tyrosine kinase (BTK)
- ImatinibBCR-ABL tyrosine kinase (ABL1 kinase domain)
- NilotinibBCR-ABL tyrosine kinase (ABL1 kinase domain)
- OsimertinibEGFR tyrosine kinase domain
- PonatinibBCR-ABL tyrosine kinase (ABL1 kinase domain), including the T315I gatekeeper mutant
- SorafenibVEGFR2 and other kinases (CRAF, BRAF, VEGFR1–3, PDGFR-β, KIT, FLT3, RET)
- VemurafenibBRAF kinase with the V600E mutation
KRAS G12C inhibitors
- About this sectionOral drugs that lock the mutant KRAS G12C protein in its «off» state; used in lung and colorectal cancers…
- AdagrasibMutant KRAS G12C (small GTPase)
- SotorasibMutant KRAS G12C (small GTPase)
MET inhibitors
- About this sectionOral selective inhibitors of the MET kinase for non-small cell lung cancer with MET exon 14 skipping. Oedema…
- CapmatinibMET (hepatocyte growth factor receptor) tyrosine kinase
- TepotinibMET (hepatocyte growth factor receptor) tyrosine kinase
Microtubule inhibitors
- About this sectionCancer drugs that jam the mitotic spindle: vinca alkaloids stop microtubules forming, taxanes freeze them…
- Cabazitaxelβ-tubulin (taxane site, inside the microtubule)
- Docetaxelβ-tubulin (taxane site, inside the microtubule)
- Eribulinβ-tubulin (vinca site, at the growing end of the microtubule)
- Ixabepiloneβ-tubulin (taxane site, inside the microtubule)
- Paclitaxelβ-tubulin (taxane site, inside the microtubule)
- Vinblastineβ-tubulin (vinca site, at the junction between tubulin dimers)
- Vincristineβ-tubulin (vinca site, at the junction between tubulin dimers)
- Vinorelbineβ-tubulin (vinca site, at the junction between tubulin dimers)
Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)
- About this sectionCancer drugs with their own mechanisms: tretinoin and arsenic make APL cells mature, asparaginase starves…
- Arsenic trioxidePML-RARα fusion protein (and other thiol-containing proteins)
- AsparaginasePlasma L-asparagine (the drug is the enzyme L-asparaginase)
- Bortezomib26S proteasome, chymotrypsin-like site (β5 subunit)
- Carfilzomib26S proteasome, chymotrypsin-like site (β5 subunit of the 20S core)
- Ixazomib26S proteasome, β5 subunit (PSMB5) of the 20S core
- PegaspargasePlasma L-asparagine (the drug is a pegylated L-asparaginase)
- TretinoinRetinoic acid receptor α (RARα), part of the PML-RARα fusion in APL
Other cancer immunotherapies (cytokines, cell vaccines, oncolytic viruses)
- About this sectionOther ways to rouse immunity against cancer: high-dose interleukin-2, a cell vaccine for prostate cancer and…
- AldesleukinInterleukin-2 receptor on T cells and NK cells
- Sipuleucel-TProstatic acid phosphatase (PAP), an antigen of most prostate cancers
- Talimogene laherparepvecMelanoma cells (infected and lysed by an engineered herpes simplex virus type 1)
PARP inhibitors
- About this sectionOral drugs that block a DNA-repair enzyme, PARP, and kill cancer cells that already lack homologous…
- NiraparibPoly(ADP-ribose) polymerases PARP1 and PARP2
- OlaparibPoly(ADP-ribose) polymerases PARP1 and PARP2
- RucaparibPoly(ADP-ribose) polymerases PARP1 and PARP2
- TalazoparibPoly(ADP-ribose) polymerases PARP1 and PARP2
PI3K inhibitors
- About this sectionOral kinase inhibitors of the PI3K-AKT pathway: alpelisib (PI3Kα) for PIK3CA-mutant breast cancer…
- AlpelisibPI3Kα, catalytic subunit p110α of phosphoinositide 3-kinase
- IdelalisibPI3Kδ, catalytic subunit p110δ of phosphoinositide 3-kinase (leukocytes)
Platinum compounds
- About this sectionCancer drugs built around a platinum atom that bind DNA and cross-link it, so tumour cells can no longer…
- CarboplatinDNA (N7 of guanine)
- CisplatinDNA (N7 of adjacent guanines)
- OxaliplatinDNA (adjacent guanines)
Selective oestrogen receptor degraders (SERDs)
- About this sectionPure antioestrogens: they block the oestrogen receptor and make the cell destroy it. Used for…
- ElacestrantOestrogen receptor alpha (ERα), ligand-binding domain
- FulvestrantOestrogen receptor alpha (ERα), ligand-binding domain
Topoisomerase inhibitors
- About this sectionCancer drugs that trap the enzymes that cut and reseal DNA. The cut DNA stays open and turns into breaks…
- EtoposideDNA topoisomerase IIα
- IrinotecanDNA topoisomerase I
- TopotecanDNA topoisomerase I
TRK and RET inhibitors (tumour-agnostic kinase inhibitors)
- About this sectionOral kinase inhibitors chosen by the tumour's gene, not its organ: larotrectinib for NTRK fusions…
- LarotrectinibTRKA, TRKB and TRKC receptor tyrosine kinases (genes NTRK1, NTRK2, NTRK3)
- SelpercatinibRET receptor tyrosine kinase (fusions and activating mutations)
VEGFR multikinase inhibitors
- About this sectionOral anti-angiogenic drugs that block VEGF receptors and other kinases; used in kidney, liver, thyroid and…
- AxitinibVEGFR1, VEGFR2 (KDR) and VEGFR3 tyrosine kinases
- CabozantinibMET, VEGFR2, RET and KIT tyrosine kinases
- LenvatinibVEGFR1-3, FGFR, PDGFR, KIT and RET tyrosine kinases
- PazopanibVEGFR1-3, PDGFR, FGFR and KIT tyrosine kinases
- RegorafenibVEGFR1-3, TIE2, PDGFR, KIT, RET, RAF1 and other kinases
- SunitinibVEGFR2 (KDR), KIT, PDGFR and other receptor tyrosine kinases
A to Z
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
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