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Discovering new cancer drugs

Drug discoveryCancer drug discovery is the process of finding or designing a molecule that has the potential to kill cancer cells or shrink tumours. Our scientists are also searching for drugs that can help prevent the development of cancer.

One of our biggest success stories is the discovery of the brain tumour drug temozolomide.

Clues from cancer biology

There is no single route to discovering a new drug. But research into cancer biology plays a huge part, as it gives scientists vital clues about potential new treatment strategies. For instance, if a certain protein is known to be involved in cancer, scientists can try to design a drug that blocks its activity.

'Structural biologists' are also important - scientists who study the shapes of molecules down to the level of individual atoms. By understanding the exact shape and size of faulty proteins in cancer cells, researchers can design drugs that will precisely fit into them - like a key in a lock.

‘Trial and error’ and the natural world

Sometimes new drugs are discovered by ‘trial and error’. Using a technique called high-throughput screening, scientists can test thousands of different chemicals until they find one that works. This can then be 'tweaked' by chemists to make it more effective.

Some drug discoveries come from the natural world. For example, the cancer drug paclitaxel (Taxol) originally came from the Pacific yew tree. And Cancer Research UK-funded scientists have been involved in the development of a new drug called Combretastatin (CA4P), which was first found in the bark of the African bush willow tree. 1, 2

Our drug discovery initiatives

A researcher working to discover new drugsCancer Research UK funds a vast array of work across the UK aimed at discovering new cancer drugs. And we are in the process of significantly expanding our drug discovery initiatives, including investing £10m in drug discovery projects at four universities across the UK.

We also have more than 80 scientists working on discovering new cancer drugs at our dedicated discovery laboratories with Cancer Research Technology.

Our pioneering work on drug discovery includes research by Paul Workman at The Institute of Cancer Research and Simon Mackay at the University of Strathclyde.

Our impact

We are world-leaders in discovering new cancer drugs, and we’ve contributed to the discovery or first trials of nearly 50 drugs now in clinical development.

Here are just a few examples of drugs now in use that we discovered:


In 1938, our scientists discovered the first artificial female hormone, diethylstilboestrol. 3 It became the treatment of choice for over 40 years for advanced prostate cancer. This work also underpinned the development of later hormone treatments, such as the prostate cancer drug bicalutamide (Casodex).

"Mustard" drugs

Our scientists were the first to realise the potential of the ‘nitrogen mustards’ as cancer drugs. In the 1950s, they discovered melphalan (Alkeran), chlorambucil (Leukeran) and busulfan (Myleran). 4-10 These drugs are still used today to treat some cases of myeloma, lymphoma and leukaemia, and have improved countless lives.

Platinum drugs

Carboplatin was discovered by our scientists in the 1980s as a result of work to improve the platinum-based drug cisplatin. 11, 12 Carboplatin has fewer side effects than cisplatin and is currently used to treat many types of cancer including ovarian, lung and testicular cancer.


Our scientists discovered temozolomide (Temodal). 13 Radiotherapy plus temozolomide is now the gold-standard of treatment for glioblastoma, one of the most common forms of adult brain tumour. Read more about the story behind temozolomide.

All our work - from research into cancer biology through to clinical trials - would not be possible without the generosity of our supporters.

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  1.  Dark, G.G. et al. Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature. Cancer Res 57, 1829-1834 (1997). PubMed link
  2. Beauregard, D.A. et al. The susceptibility of tumors to the antivascular drug combretastatin A4 phosphate correlates with vascular permeability. Cancer Res 61, 6811-6815 (2001). PubMed link
  3.  Dodds, E.C. Oestrogenic activity of certain synthetic compounds. Nature 247-248 (1938). Link to paper
  4.  Haddow, A., Kon, G.A.R. & Ross, W.C.J. Effects upon tumours of various haloalkylarylamines. Nature 162, 824-825 (1948). Link to paper
  5. Goldacre, R.J., Loveless, A. & Ross, W.C.J. Mode of production of chromosome abnormalities by the nitrogen mustards: the possible role of cross-linking. Nature 163, 667-669 (1949). Link to paper
  6. Everett, J.L., Roberts, J.J. & Ross, W.C.J. Aryl-2-halogenoalkylamines. Part XII. Some carboxylic derivatives of NN-di-2-chloroethylaniline J Chem Soc, 2386-2392 (1953).
  7. Haddow, A. & Timmis, G.M. Myleran in chronic myeloid leukaemia; chemical constitution and biological action. Lancet 264, 207-208 (1953). PubMed link
  8. Bergel, F. & Stock, J. Annual Report. British Empire Cancer Campaign 31, 6 (1953).
  9. Bergel, F. & Stock, J.A. Cytoactive amino-acid and peptide derivatives. Part I. Substituted phenylalanines. J Chem Soc, 2409-2417 (1954).
  10. Bergel, F. Design of alkylating agents for selectivity of action. Ann N Y Acad Sci 68, 1238-1245 (1958). PubMed link
  11.  Calvert, A.H. et al. Early clinical studies with cis-diammine-1,1-cyclobutane dicarboxylate platinum II. Cancer Chemother Pharmacol 9, 140-147 (1982). PubMed link
  12. Kelland, L.R. et al. Mini-review: discovery and development of platinum complexes designed to circumvent cisplatin resistance. Journal of Inorganic Biochemistry 77, 111-115 (1999). PubMed link
  13.  Stevens, M.F.G. et al. Antitumor activity and pharmacokinetics in mice of 8-carbamoyl-3-methyl-imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (CCRG 81045; M & B 39831), a novel drug with potential as an alternative to dacarbazine. Cancer Res 47, 5846-5852 (1987). PubMed link
Updated: 25 September 2009