|Trade names||CeeNU, Gleostine, CCNU, others|
|Drug class||Alkylating agent|
|Main uses||Brain tumors, melanoma, Hodgkin lymphoma (HL)|
|Side effects||Pulmonary fibrosis, low platelets, low white blood cells, low red blood cells, nausea, kidney problems, liver problems|
|By mouth (capsules)|
|Metabolites||Monoxydroxylated metabolites, trans-4-hydroxy-CCNU, cis-4-hydroxy-CCNU|
|Elimination half-life||16–48 hours (metabolites)|
|Chemical and physical data|
|Molar mass||233.70 g·mol−1|
|3D model (JSmol)|
|Melting point||90 °C (194 °F)|
|(what is this?)|
Lomustine sold under the brand name CeeNU, is a medication used to treat brain tumors, melanoma, and Hodgkin lymphoma (HL). In HL it is used when other treatments have not worked. It is taken by mouth.
Common side effects include pulmonary fibrosis, low platelets, low white blood cells, low red blood cells, nausea, kidney problems, and liver problems. Other side effects may include hair loss, confusion, vision loss, and mouth inflammation. It should not be used in pregnancy or breastfeeding. It is an alkylating nitrosourea compound.
Lomustine was approved for medical use in the United States in 1976. It is available as a generic medication. In the United States it costs about 1,050 USD per 100 mg pill as of 2021. This amount in the United Kingdom costs the NHS about £50.
By itself it is used at a dose of around 120 to 130 mg/m2 every 6 to 8 weeks.
Mechanism of action
It is closely related to semustine and is in the same family as streptozotocin. It is a highly lipid-soluble drug, thus it crosses the blood-brain barrier. Lomustine has a long time to nadir (the time when white blood cells reach their lowest number). It is a monofunctional alkylating agent, alkylates both DNA and RNA, has the ability to cross-link DNA. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins. Lomustine is cell-cycle nonspecific.
Society and culture
In the U.S., the patent for lomustine has expired, but only one company manufactures it. In 2013, Bristol-Myers Squibb Co. sold its CeeNU brand of lomustine to CordenPharma, a subsidiary of International Chemical Investors S.E., which markets it as Gleostine through NextSource Biotechnology. In 2013, BMS charged $50 a capsule. In 2018, NextSource charged $768 a capsule. Some doctors said the price increase made it unaffordable, and one doctor called it "price gouging."
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