chembl-universe

Abarelix was the first GnRH antagonist for prostate cancer, approved in the United States in 2003 for men who could not take agonists, but allergic reactions restricted it and it was withdrawn from the US market in 2005; it remained available in Germany.

Alitretinoin gel is a vitamin A derivative applied directly to Kaposi sarcoma skin lesions in people with AIDS, approved in the United States in 1999 as the first topical treatment for the disease.

Altretamine is an oral chemotherapy tablet approved in 1990 as a single agent for ovarian cancer that has persisted or come back after platinum-based treatment, now rarely used.

Aminoglutethimide produced a medical adrenalectomy for advanced breast and prostate cancer in the 1970s and 1980s, the ancestor of today's aromatase inhibitors, and was withdrawn once selective drugs arrived.

Amsacrine is an intravenous leukaemia drug, approved in Europe, Canada and Australia in the 1980s, used mainly for acute myeloid leukaemia that has relapsed or resisted anthracycline-based treatment.

Buserelin is one of the original GnRH agonists, approved in Europe and Canada in the 1980s for advanced prostate cancer and also used in endometriosis and fertility treatment; it is not sold in the United States.

Choline C-11 was the first PET tracer approved in the United States, in 2012, to find where prostate cancer has come back when PSA rises after treatment; PSMA tracers have now largely replaced it.

Cinacalcet is a tablet that quiets overactive parathyroid tissue, approved in 2004 and labelled for the dangerous high calcium levels of parathyroid carcinoma, a rare cancer where surgery often cannot remove all the hormone-producing tissue.

Diethylstilbestrol was the first hormonal treatment for prostate cancer, standard from the 1940s, and was also given for breast cancer, before its cardiovascular harms and the cancers it caused in the daughters of women who took it in pregnancy ended its use.

Dolasetron is one of the serotonin-blocking antiemetics that transformed chemotherapy in the 1990s, approved in 1997 to prevent nausea and vomiting; its intravenous form lost its chemotherapy indication in 2010 because of heart rhythm effects.

Doxifluridine is an oral fluorouracil prodrug approved in Japan in 1987 and used in China and Korea for stomach, bowel and breast cancers; capecitabine, which the body turns into doxifluridine, later carried the same idea to the rest of the world.

Dronabinol is synthetic THC in a capsule, approved in 1985 for chemotherapy nausea and vomiting that other antiemetics have failed to control, and later for appetite loss in AIDS; it sits well behind the 5-HT3 and NK1 antagonists in today's guidelines.

Eflapegrastim is a once-per-cycle white cell growth factor approved in the United States in 2022 to prevent infections when chemotherapy for solid tumours knocks down neutrophils, an alternative to pegfilgrastim.

Estramustine is an oral prostate cancer drug that combines an oestrogen with an alkylating agent, approved in the United States in 1981 for metastatic disease and later combined with taxanes, though its clotting risk has pushed it out of routine use.

Lipiodol is an iodine-rich oil injected into the liver's artery that lodges in liver tumours; it lets radiologists see them on CT and is the vehicle that carries chemotherapy into the tumour in conventional chemoembolisation for liver cancer.

Floxuridine is a cousin of fluorouracil pumped directly into the liver's artery to treat bowel cancer that has spread to the liver, delivering a very high local dose with little reaching the rest of the body.

Fluoxymesterone is an oral male hormone approved in 1956 and once used to palliate advanced breast cancer in women, an approach abandoned when better tolerated antioestrogens and aromatase inhibitors arrived.

Formestane, launched in Europe in 1993, was the first selective aromatase inhibitor for advanced breast cancer, given by injection every two weeks; oral exemestane and the non-steroidal inhibitors made it redundant within a few years.

Hexaminolevulinate makes bladder tumours fluoresce red under blue light so the urologist can see and remove flat and tiny cancers that white-light cystoscopy misses.

Histrelin is a GnRH agonist delivered by a small implant under the skin of the arm that lasts a whole year, approved in the United States as Vantas for palliative treatment of advanced prostate cancer and as Supprelin for early puberty in children.

Infigratinib is an FGFR inhibitor pill given accelerated approval in the United States in 2021 for bile duct cancer with an FGFR2 fusion, then withdrawn in 2024 when its confirmatory trial could not enrol; it is now being developed for achondroplasia instead.

Lenograstim is Europe's and Japan's glycosylated form of G-CSF, given after chemotherapy to shorten the period of dangerously low neutrophils and to mobilise stem cells for transplant; it does the same job as filgrastim.

Uvadex is the drug used in photopheresis, where a patient's white cells are drawn off, treated with methoxsalen and ultraviolet light, and returned; it is approved for the skin symptoms of cutaneous T-cell lymphoma and widely used for graft-versus-host disease.

Methyl aminolevulinate is a cream applied to sun-damaged skin or a superficial basal cell carcinoma and then activated with red light, clearing precancerous and early skin cancers with better cosmetic results than surgery or freezing.

Mitobronitol was a Hungarian-developed oral tablet used in Europe from the 1960s to control chronic myeloid leukaemia and polycythaemia, an alternative to busulfan that disappeared once hydroxycarbamide, interferon and imatinib took over.

Motixafortide is an injection given with G-CSF before stem cell collection in people with multiple myeloma, approved in the United States in 2023, so that enough stem cells for an autologous transplant can be harvested in one or two sessions.

Nabilone is a synthetic cannabinoid capsule approved in 1985 for chemotherapy-induced nausea and vomiting that standard drugs cannot control; like dronabinol it is a later-line option because of its effects on mood and balance.

Nedaplatin is a Japanese platinum drug, approved there in 1995, used for head and neck, oesophageal, lung, cervical and other squamous cancers as a gentler alternative to cisplatin on the kidneys; it has never been approved in the West.

Nimotuzumab is a Cuban-developed antibody against EGFR approved in India, China, Cuba and other countries for head and neck cancer, nasopharyngeal cancer and brain tumours, usually with radiotherapy; it causes far less rash than cetuximab but has never been approved in the United States or Europe.

Olaratumab was approved in 2016 with doxorubicin for soft tissue sarcoma after a small trial suggested it added almost a year of life, but the large confirmatory trial found no benefit and it was withdrawn in 2019, a warning case for accelerated approvals.

Olmutinib was a Korean-developed EGFR pill approved in South Korea in 2016 for lung cancers that had developed the T790M resistance mutation, the same niche as osimertinib; severe skin reactions and osimertinib's success ended its development.

Oprelvekin was the first drug approved, in 1997, to prevent the severe platelet falls that chemotherapy causes, but fluid retention and heart rhythm problems limited it and it was withdrawn in 2011; thrombopoietin agonists took over the problem.

Peginterferon alfa-2b, a long-acting interferon, was approved in 2011 as Sylatron for melanoma that had spread to lymph nodes and been removed, to delay recurrence; checkpoint inhibitors have since replaced it in that role.

Pipobroman was an oral tablet approved in 1966 for polycythaemia vera, the blood disorder that makes too many red cells, and for chronic myeloid leukaemia; it was discontinued after studies showed it raised the risk of leukaemia compared with hydroxycarbamide.

Pixantrone is an anthracycline-like drug engineered to spare the heart, approved in the European Union in 2012 as a single agent for adults with aggressive B-cell lymphoma that has relapsed several times.

Plicamycin, approved in 1970, was a chemotherapy for testicular cancer that fell out of use as cisplatin arrived, and was kept for treating dangerously high calcium levels caused by cancer until it was discontinued in 2000.

Plitidepsin is a chemotherapy derived from a Mediterranean sea squirt, approved in Australia in 2018 with dexamethasone for multiple myeloma after several other treatments; the European regulator refused it, and it drew attention in 2021 as a possible COVID-19 antiviral.

Porfimer sodium is the drug half of photodynamic therapy: injected, it gathers in tumours, and a laser passed through an endoscope two days later activates it to burn away oesophageal and lung tumours that block the airway or gullet.

Raltitrexed is a three-weekly intravenous antifolate used in Europe, Canada and Australia for advanced bowel cancer, and with cisplatin for mesothelioma, in patients who cannot take fluorouracil.

Sargramostim is a lab-made version of GM-CSF, the signal that tells bone marrow to make white cells; approved in 1991, it shortens the dangerous low-count period after leukaemia chemotherapy and stem cell transplants.

Streptozocin is a chemotherapy drug that seeks out pancreatic islet cells, approved in 1982 for the rare tumours that arise from them; the same selectivity makes it the standard way to induce diabetes in laboratory animals.

Technetium sulfur colloid is the radioactive tracer injected around a breast cancer or melanoma before surgery so the surgeon can find the first lymph node the tumour drains to and remove only that node instead of the whole basin.

Teniposide is a close relative of etoposide approved in the United States in 1992 for children whose acute lymphoblastic leukaemia has come back after induction, and used in Europe for childhood brain tumours and neuroblastoma.

Trilaciclib is given as an infusion just before chemotherapy for small cell lung cancer to put the bone marrow's stem cells briefly to sleep, so fewer are killed and patients need fewer transfusions and growth factor injections.

Uracil mustard was an oral alkylating agent approved in 1962 for chronic lymphocytic leukaemia and lymphomas, one of the early nitrogen mustard tablets, and long since discontinued.

Vindesine is a vinca alkaloid, a semi-synthetic relative of vinblastine, used in Europe and elsewhere for acute lymphoblastic leukaemia and some solid tumours; it was never marketed in the United States.