What Is Lomustine? Uses, Dosage, and What You Need to Know in 2026

Lomustine is an oral chemotherapy drug that has been treating brain cancer and lymphoma for nearly 50 years. Despite being one of the oldest oncology medications still in regular use, it remains clinically essential — particularly for brain tumor patients for whom very few oral chemotherapy options exist. Here's a complete overview of what lomustine is, how it works, how it's taken, and what patients should know in 2026.

What Is Lomustine?

Lomustine is the generic name for the drug also known by:

Gleostine — the current brand name (NextSource Biotechnology)

CeeNU — discontinued brand name (Bristol-Myers Squibb, discontinued 2013)

CCNU — chemical abbreviation used widely in oncology literature

It belongs to a drug class called nitrosourea alkylating agents. First approved by the FDA in 1977, lomustine is one of the oldest chemotherapy drugs still routinely prescribed and is considered standard of care for recurrent glioblastoma in many guidelines.

What Is Lomustine Used For?

FDA-approved indications for lomustine:

Brain tumors (primary and metastatic) in patients who have already received surgery and/or radiation — including glioblastoma (GBM), anaplastic astrocytoma, and other malignant gliomas

Hodgkin's lymphoma (secondary/salvage therapy) in patients who relapsed after or failed primary treatment

Off-label and international uses include non-Hodgkin lymphoma, melanoma (in some countries), and lung cancer. Lomustine is also used in veterinary oncology for cats and dogs.

What Makes Lomustine Unique Among Chemotherapy Drugs?

Three properties make lomustine uniquely valuable for brain tumors:

It crosses the blood-brain barrier. Most chemotherapy drugs cannot reach the brain because the blood-brain barrier blocks them. Lomustine's high lipid solubility allows it to pass through this barrier and reach tumor cells in the brain.

It's taken by mouth. Unlike many cancer treatments that require IV infusions at a clinic, lomustine is an oral capsule taken at home. This improves patient convenience significantly.

It's cell-cycle non-specific. Lomustine damages cancer cells regardless of where they are in the cell division cycle, meaning it can affect rapidly and slowly dividing cancer cells alike.

How Is Lomustine Taken? Dosage and Administration

Dose: 130 mg/m² (based on body surface area) as a single oral dose every 6 weeks; reduced to 100 mg/m² for patients with bone marrow compromise

Capsule strengths: 5 mg (yellow), 10 mg (white), 40 mg (white/green), 100 mg (green)

Administration: All capsules for the dose are taken at once, on an empty stomach (at least 2 hours after eating), ideally at bedtime to minimize nausea

Handling: Wear gloves; do not break, crush, or open capsules

Dispensing: Only one dose dispensed at a time by the pharmacy to prevent accidental overdose

Is Lomustine a Controlled Substance?

No. Lomustine is not classified as a controlled substance by the DEA. It does not have abuse potential. However, it is tightly regulated in terms of dispensing (one dose at a time) because of its high toxicity and the risk of fatal overdose.

Key Safety Information

Boxed warning: Delayed, cumulative, and potentially fatal myelosuppression — blood counts must be monitored weekly for at least 6 weeks after each dose

Never take more often than every 6 weeks — this is a hard rule due to cumulative bone marrow toxicity

Avoid pregnancy: Can cause serious fetal harm; women must use contraception during and 2 weeks after treatment; men must use contraception for 3.5 months after treatment

Availability and Cost in 2026

Lomustine is available but not always easy to find. It is not stocked at most retail pharmacies, not covered by Medicare or Medicaid, and costs $600–$2,950 per dose at retail prices. Patient assistance programs, discount cards, and specialty pharmacies are the primary access channels. See our related posts for more on finding and affording lomustine:

How to find lomustine in stock near you | How to save money on lomustine | Search with medfinder