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Ломустин

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Ломустин

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Ломустин

What is Lomustine?

Lomustine is an alkylating agent belonging to the nitrosourea family of compounds. It is a specialized chemotherapy medication used primarily in the treatment of certain types of cancer. Due to its chemical properties, lomustine is lipid-soluble, which allows it to cross the blood-brain barrier—a protective membrane that prevents many other substances and medications from entering the central nervous system.

Mechanism of Action

As an alkylating agent, lomustine works by interfering with the replication of DNA within rapidly dividing cells. It attaches an alkyl group to the DNA strands, leading to cross-linking and strand breakage. These structural changes prevent the cancer cells from successfully dividing and multiplying. Because cancer cells typically divide more frequently than healthy cells, they are more susceptible to this type of interference.

Primary Uses

Lomustine is most frequently utilized in oncology for the management of the following conditions:

  • Brain Tumors: It is often employed to treat both primary brain tumors and metastatic lesions that have spread to the brain from other parts of the body.
  • Hodgkin Lymphoma: It may be used as part of a treatment regimen for patients with Hodgkin disease, particularly when the disease has progressed after initial treatments or in cases of relapse.

Characteristics

Unlike many other chemotherapy treatments that require intravenous administration in a clinical setting, lomustine is administered orally. This allows the medication to be absorbed through the digestive system before it enters the bloodstream to target malignant cells throughout the body.

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What side effects are possible with Ломустин?

Possible Side Effects and Safety Information

The safety profile of Lomustine (CCNU) is characterized by specific, officially documented adverse reactions and safety constraints derived from government regulatory labeling, such as the FDA and EMA SmPC. The most critical and dose-limiting adverse effect is delayed bone marrow suppression (myelosuppression).

Officially Documented Adverse Reactions

Adverse effects are categorized by System-Organ Class (SOC) and frequency based on regulatory standards. Safety classifications may vary by region.

System-Organ Class (SOC) Frequency Classification Official Adverse Reaction Listing
Blood and Lymphatic Most Frequent / Cumulative Delayed Myelosuppression (Thrombocytopenia, Leukopenia)
Gastrointestinal Very Common Nausea, Vomiting, Decreased appetite
Hepatobiliary Common to Rare Hepatic function abnormal, Jaundice, Hepatic failure
Respiratory Rare Pulmonary fibrosis, Interstitial lung disease
Renal and Urinary Uncommon Renal failure, Renal injury

Serious Safety Considerations

Serious adverse reactions documented in regulatory sources include:

  • Delayed and Cumulative Myelosuppression: The primary risk is dose-related bone marrow toxicity, with nadirs typically occurring 4 to 6 weeks after administration, necessitating close monitoring.
  • Organ Toxicities: There is a documented risk of severe, dose-related Pulmonary Toxicity and Nephrotoxicity associated with long-term use and high total cumulative doses.
  • Secondary Malignancies: The drug is associated with a risk of developing secondary acute leukemia and myelodysplasia.

Population-Specific Safety Notes

  • Pregnancy and Fertility: Lomustine is contraindicated during pregnancy due to a high risk of fetal harm (teratogenicity). It can also cause impaired fertility and permanent sterility in both male and female patients.
  • Contraindications: Use is restricted in patients with known hypersensitivity to nitrosoureas, severe bone marrow depression, or severe renal impairment.
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Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory information emphasizes that overdosage with Lomustine can cause fatal toxicity and is associated with an increased severity of documented adverse effects.

Immediate medical attention is required if there is any suspicion of an overdose, as symptoms of toxicity may be severe and progress rapidly.

Documented Overdose Manifestations

System Manifestations
Hematologic Heightened and delayed myelosuppression (bone marrow toxicity)
Gastrointestinal Abdominal pain, vomiting, diarrhea, anorexia
Systemic Lethargy (extreme fatigue/dizziness), multiple organ failure (in very severe cases)
Hepatic/Pulmonary Abnormal hepatic function, cough, and shortness of breath

Emergency Actions

There is no specific antidote for Lomustine overdose. Treatment is focused on immediate intervention and supportive care.

Immediate actions required by medical personnel include:

  • Gastric Lavage: Overdose should be treated immediately by gastric lavage.
  • Supportive Care: Treatment is symptomatic and supportive. This includes taking appropriate measures for blood product replacement when clinically indicated.
  • Infection Control: Supportive measures such as infection prophylaxis should be instituted due to the risk of severe myelosuppression.

If you believe the acceptable dose has been exceeded, you must immediately contact an emergency room or toxicology center for urgent medical care. The risk of fatal toxicity is increased by dispensing or administering more than one single dose at a time.

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Therapeutic Uses of Ломустин

What Ломустин treats: main uses and benefits

Lomustine is primarily used to help manage the advancement of malignant gliomas (such as glioblastoma and anaplastic astrocytoma) and secondary brain metastases. The drug is generally applied in conditions characterized by periods of heightened symptoms, following appropriate surgical and/or radiotherapeutic procedures. Its use is applicable in the CNS, where it addresses symptoms related to tumors in that location, which may assist with easing the intensity of related neurological symptoms caused by the tumor mass. The medication is also considered a relevant therapeutic option for cancers that have either returned after initial treatment or have shown resistance to prior cytotoxic agents, and is considered relevant for managing Hodgkin's lymphoma.

“The goal of this therapy is to provide supportive assistance during difficult symptomatic phases and contribute to the management of the overall symptom load.”

This supportive secondary treatment path assists with managing symptoms related to temporary physiological imbalance and is relevant for supporting appropriate symptomatic management when integrated into combination protocols.

Quick Fact Description
Primary Use Management of malignant brain tumors and specific lymphomas.
Clinical Scenario Used following initial treatments or for relapsed/refractory disease.
Key Benefit Contributes to easing the overall symptom load by supporting the management of symptomatic manifestations.
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Eligibility and Restrictions for Use

Lomustine (also known as CeeNU or Gleostine) is typically prescribed as part of a chemotherapy regimen for treating primary and metastatic brain tumors and refractory or relapsed Hodgkin’s lymphoma.

Who Cannot Use Lomustine (Contraindications)

Lomustine is generally contraindicated and should not be used in the following situations due to the risk of severe or life-threatening complications:

Condition Reason for Restriction
Previous Hypersensitivity Any known severe allergic reaction to lomustine
Pregnancy High risk of fetal harm (teratogenicity and embryotoxicity)
Breastfeeding Drug may pass into breast milk
Concurrent Live Vaccines Risk of developing the infection due to an immunosuppressed state

Use with Caution (Warnings and Precautions)

Close medical supervision and potential dose adjustments are necessary for patients with pre-existing conditions that can be worsened by the drug's primary toxicities, particularly its delayed and cumulative bone marrow suppression.

Your healthcare provider must be informed if you have or have recently had:

  • Existing Myelosuppression: Low blood cell counts (leukopenia, thrombocytopenia, or anemia) from prior treatments.
  • Impaired Organ Function: Severe kidney or liver dysfunction.
  • Pre-existing Lung Disease: Increased risk of pulmonary toxicity.

Women of childbearing potential and male patients must use effective contraception during and for a period following treatment, as lomustine can cause harm to a developing fetus and affect fertility.

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What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile is based strictly on official regulatory documentation and is categorized by effect.

Interaction Scope

Category Official Regulatory Documentation
Medicinal product categories with documented interactions: Live Vaccines, Other Cytostatics, Enzyme-inducing Antiepileptic Drugs, Enzyme Inhibitor Drugs, H2-receptor antagonists.
Specific interacting medicines (if explicitly listed): Phenobarbital, Theophylline, Cimetidine, Valproic Acid.
Mechanistic basis of interactions (only if stated in label): Pharmacokinetic interaction (microsomal liver enzyme induction and inhibition); Pharmacodynamic interaction (potentiation of myelotoxicity/bone marrow depression).
Interaction-related restrictions: Contraindicated co-administration of Live Vaccines.

Interaction Classifications (High-Level)

Category Official Regulatory Documentation
Interaction severity classification (as defined in official documents): Contraindicated (Live Vaccines); Use with Caution/Monitoring (Antiepileptics, Cimetidine).
Regulatory basis (EMA / FDA / etc.): Information is based strictly on government regulatory sources, such as the Summary of Product Characteristics (SmPC) and FDA labeling.
Interaction-context constraints (as defined in official documents): Immune status (Contraindicated in immunosuppressed patients); Combination therapy (Risk with other cytostatics and radiation therapy).

Resulting Interaction Structure

Official Interaction Statements:

  • Live Vaccines are contraindicated in immunosuppressed patients due to the documented risk of fatal systemic vaccinal disease.
  • Co-administration with Phenobarbital causes microsomal liver enzyme induction, which leads to accelerated elimination and a reduced antitumour effect.
  • The co-administration of Theophylline or Cimetidine may potentiate bone marrow toxicity.
  • Enzyme-inhibiting drugs, such as Valproic Acid, may impair metabolism and potentially increase toxicity.
  • Concomitant treatment with Other Cytostatics or Radiation Therapy can increase the bone marrow depression effect.

Connection to the overall interaction profile (2–4 sentences):

The regulatory profile defines the drug’s interaction structure around three primary concerns: strict prohibition of live vaccines, pharmacokinetic alteration with enzyme-modifying drugs, and pharmacodynamic potentiation of myelosuppression when combined with other cytotoxic agents or specific H2-receptor antagonists. This structure identifies constraints necessary to manage the risk of reduced efficacy or increased toxicity, based solely on documented official data.

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Mechanism of Action

How Ломустин works: Mechanism of Action

Ломустин (Lomustine) is a highly lipophilic prodrug that readily crosses the blood-brain barrier (BBB), exerting its primary effects centrally and peripherally. Once metabolized, it yields two active agents: an alkylating agent and a carbamoylating agent.

The alkylating agent forms permanent covalent bonds with DNA bases, leading to interstrand cross-links (ICLs) that physically prevent DNA strand separation. The carbamoylating agent modifies and inhibits the function of key cellular proteins.

This severe, unrepaired molecular damage activates DNA damage response checkpoints, forcing the cell into G2/M cycle arrest. This failure to progress through division triggers the intrinsic apoptotic cascade, inducing programmed cell death. A resulting physiological consequence of this non-specific cytotoxicity is the modulation of hematopoiesis due to the effect on actively dividing bone marrow progenitor cells.

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Dosage and Administration Information

Official Administration Guidelines

Lomustine (also known as CCNU) is a medication administered according to a strict, cyclical regimen based on official regulatory instructions.

Route and Frequency

The medication is available as hard capsules and is administered by the oral route (swallowed). Lomustine must be taken as a single, complete dose for one course of treatment. Subsequent doses must not be given more frequently than every six weeks (42 days).

Dosing Schedule and Administration Conditions

The standard starting dose is 130 mg/m^2 of body surface area for adults and pediatric patients, often reduced to 100 mg/m^2 in patients with compromised bone marrow function. The total dose may consist of different capsule strengths (e.g., 5 mg, 10 mg, 40 mg, 100 mg), and all capsules must be swallowed whole with water. They must not be crushed, opened, or chewed. The drug is preferably taken on an empty stomach.

Procedural Requirements

  1. Single Dose: The patient takes the calculated dose as a single unit on the scheduled day.
  2. Monitoring: Following administration, blood counts must be monitored weekly for at least six weeks to determine the nadir (lowest) counts.
  3. Subsequent Dosing: The dose for the next cycle is strictly conditional. It is given only after the minimum 6-week interval has passed and the blood counts have recovered to acceptable levels (e.g., platelet count ge 100,000/mm^3 and leukocyte count ge 4,000/mm^3). The next dose must be adjusted downward if the prior nadir counts were too low, defining the cumulative and recovery-dependent nature of the drug's use protocol.

Note: Healthcare professionals must only dispense enough capsules for one single treatment dose.

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Recent Clinical Evidence

Research Evidence / Overview of Studies for Ломустин (Lomustine)


Evidence for Use in Primary Brain Tumors (e.g., Glioblastoma)

Clinical studies have studied Ломустин (Lomustine) in the research setting of primary brain tumors, which are often associated with functional limitations. Research has evaluated the compound alone and with other interventions, focusing on outcomes reflecting daily functioning and systemic imbalance. Studies report patterns of change in measured outcomes, but the results apply only to the studied populations. Findings have been mixed in some reviews, and comparative evidence is lacking in certain areas.


Evidence for Use in Hodgkin's Lymphoma

Ломустин was studied in the research setting of Hodgkin's lymphoma, a condition characterized by fluctuating manifestations. These investigations explored changes in outcomes related to systemic imbalance, often after other interventions. Data show patterns related to changes in the condition observed in some studies. However, the evidence base is limited, often featuring modest sample sizes, meaning the certainty remains low, and data are still emerging from contemporary research settings.


Long-term Studies and Follow-up

Research examined the patterns of change observed during initial treatment and tracked patient-reported outcomes over extended follow-up durations. Studies report how symptoms evolved in observed populations over time. It is important to know that long-term effects are not fully established. Follow-up durations were limited in many key studies, meaning there is limited information for outcomes that occur many years after initial evaluation.


Evidence in Special Populations

Ломустин was evaluated in special populations, including children and older adults, to understand if observed patterns differ. Research explored outcomes related to systemic imbalance in these groups. Subgroup findings are uncertain due to smaller participant numbers. Data for children and individuals with comorbid conditions (e.g., liver or kidney issues) remain insufficient, and the results apply only to the populations studied.


What is Still Uncertain About Ломустин

Research is ongoing to address the evidence gaps. Main uncertainties relate to the long-term patterns, as long-term effects are not fully established, and comparative evidence is lacking in several areas of care. Inconsistencies exist where findings were mixed across studies. Research provides context but not individual predictions, and continued study focuses on filling these gaps in the broader evidence landscape.

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Frequently Asked Questions (FAQ)

Common questions about Ломустин (FAQ)

Q: How does Ломустин compare generally to other similar cancer medicines?

A: Regulatory documents classify Ломустин as an alkylating agent belonging to the nitrosourea class. A key distinction noted in official information is the drug's high lipid solubility. This physical property allows it to effectively cross the blood-brain barrier, which is a feature that influences its clinical use for certain central nervous system tumors.

Q: Why is Ломустин sometimes given in cycles instead of daily?

A: Ломустин is administered in cycles with a mandatory minimum interval between doses, typically no more frequently than every six weeks. This schedule is necessary because the drug's primary side effect, low blood counts (myelosuppression), is delayed and cumulative. The time between doses allows the patient's blood counts a period of recovery before the next course is permitted.

Q: Do side effects from Ломустин start immediately after taking it?

A: Side effect onset varies depending on the type of reaction. Common gastrointestinal issues like nausea and vomiting may occur relatively quickly, often within 3 to 6 hours after swallowing the capsules. However, the most serious adverse effect, the drop in blood counts, is delayed and typically does not begin until 4 to 6 weeks after administration.

Q: How long do the side effects of Ломустин typically last?

A: Common effects such as nausea and vomiting generally resolve quickly, often lasting less than 24 hours. For the dose-limiting toxicity of low blood counts (leukopenia and thrombocytopenia), the nadir (lowest point) is reached around 4 to 6 weeks after the dose. The official documentation indicates that counts usually persist at this low level for approximately one to two weeks before beginning to recover.

Q: What do official documents say about the use of Ломустин in older adults?

A: Official labeling advises caution when selecting a dose for older adults. Regulatory texts note that this population is more likely to have reduced kidney function. Since the drug is processed and excreted by the kidneys, the risk of toxic reactions may be greater, and monitoring of kidney function may be warranted for older adults.

Q: How long can Ломустин cause long-term health problems?

A: Long-term effects have been reported to occur months or years after treatment is initiated. For example, pulmonary toxicity (lung damage) has been reported to appear as late as 15 years after the initial course of therapy. Furthermore, the drug is officially associated with an increased risk of secondary cancers (such as acute leukemia) with long-term, cumulative use.

Q: Does Ломустин interact with common pain relievers like Tylenol (paracetamol)?

A: Official information explicitly states that Ломустин is associated with the risk of liver injury (hepatotoxicity). Because some nonprescription pain relievers, such as acetaminophen (paracetamol), can also affect the liver, official guidelines advise that all medications taken should be disclosed to the healthcare team, as monitoring may be necessary.

Q: Can I take multivitamins while undergoing treatment with Ломустин?

A: Patient-facing information derived from regulatory documents advises that the treating physician should be informed of all products being taken. This includes prescription and nonprescription medicines, vitamins, nutritional supplements, and herbal products. Regulatory guidance emphasizes the importance of informing the treating physician of all products being taken so that potential interactions can be evaluated.

Q: Are there any foods or supplements that should be avoided while taking Ломустин?

A: Official administration instructions state that the medicine is preferably taken on an empty stomach, which may help minimize nausea and vomiting. Regarding supplements, official guidance emphasizes informing the healthcare provider of all herbal products and supplements being used, allowing for evaluation of potential interaction risks.

Q: What does official documentation say about using Ломустин if a person has kidney issues?

A: The official product information lists that the drug can cause kidney damage (nephrotoxicity) and progressive renal failure has been reported. Since the kidneys are responsible for eliminating the drug, patients with existing impaired kidney function may have an increased risk of severe toxic reactions. Kidney function monitoring is advised, and dose adjustments may be considered based on the patient's condition.

Q: Do people gain or lose weight while on Ломустин?

A: Official adverse reaction listings include common gastrointestinal effects such as nausea, vomiting, and decreased appetite. While regulatory documents do not directly state that people gain or lose weight, they do link treatment to factors that influence eating and nutrition, which can subsequently impact body weight.

Q: Is Ломустин a standard first-line treatment for its approved uses?

A: The FDA labeling describes the use of Ломустин as treatment for certain primary and metastatic brain tumors. For Hodgkin’s lymphoma, it is indicated for disease that is refractory (has not responded) or has relapsed following initial therapy. This positioning suggests its use is often reserved for situations where first-line treatments have not been successful.

Q: Does Ломустин have an official drug warning or 'Black Box' warning?

A: Yes, the drug's official labeling includes a Boxed Warning, often referred to as a Black Box Warning, to highlight the most serious risks associated with its use. This warning specifically calls attention to the delayed, cumulative, and dose-related toxicity to the bone marrow (myelosuppression), which can lead to potentially fatal infections or bleeding.

Q: Are there specific symptoms that require immediate medical attention while on Ломустин?

A: Patient-facing safety documents list several symptoms that are listed as requiring urgent reporting to the healthcare team. These include signs of infection (like fever, chills, or sore throat), unusual bleeding or bruising, jaundice (yellowing of the skin or eyes), and new or worsening respiratory issues such as cough or shortness of breath.

Q: Can the side effects of Ломустин be managed with other medicines?

A: Official regulatory documents acknowledge that supportive medications can be used to manage certain side effects. Specifically, antiemetics (anti-nausea medicines) administered before taking Ломустин have been noted to be effective in diminishing or preventing common gastrointestinal side effects like nausea and vomiting.

Q: Is Ломустин often given with anti-nausea medication?

A: Due to the common occurrence of nausea and vomiting, the official label notes that prior administration of antiemetics (anti-nausea medicines) is effective. This pre-treatment is a common practice to help reduce the severity of these gastrointestinal adverse reactions.

Q: Why is the drug dosing based on body surface area?

A: Like many chemotherapy drugs, Ломустин is dosed based on the patient's body surface area (BSA), measured in square meters (m^2). This method is used because BSA is considered a more reliable measure than body weight alone for calculating the dosage needed to achieve the proper drug concentration relative to the patient's overall physiological factors, such as cardiac and renal function.

Q: What is the chemical structure of Ломустин described as in scientific literature?

A: In scientific and regulatory literature, the active ingredient, Ломустин, is chemically described by its IUPAC name: 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea. Its molecular formula is officially designated as C9H16ClN3O2.

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How should Ломустин be stored and disposed of?

How to Store and Dispose of Lomustine (Ломустин)

Official regulatory guidelines mandate specific conditions for storing and disposing of Lomustine capsules. The medicine must be stored at controlled room temperature, typically between 20 C and 25 C (68 F and 77 F), and must be protected from both light and moisture. It is strictly prohibited to freeze the medication, and it should remain in its original, tightly closed container.

Due to the drug's cytotoxic classification, special handling precautions are required, including wearing gloves and avoiding the crushing or opening of capsules. The product must always be stored securely out of the reach of children and pets. Unused or expired Lomustine must not be discarded in household trash, down the sink, or into the toilet. Disposal must follow local regulations for hazardous or cytotoxic pharmaceutical waste.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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