Gleostine

Quick links to important sections

Gleostine

Selected form

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.

Overview of Gleostine

Property Description
Active ingredient Lomustine (INN)
Form Capsules (solid oral dosage form)
Pharmacological class Antineoplastic Alkylating Agent
General purpose To inhibit the growth and reproduction of malignant cells
Origin Synthetic compound (nitrosourea)

Gleostine is the brand name for the prescription-only synthetic medication Lomustine (INN), which is classified as a cytotoxic antineoplastic agent. It belongs to the specific nitrosourea class of chemotherapy drugs, functioning primarily as an alkylating agent. The medication's core therapeutic purpose is to attack and prevent the rapid and abnormal multiplication of malignant cells in the body.

What Type of Chemotherapy is Gleostine (Lomustine)?

The active substance, Lomustine, is a synthetic compound that acts as a cell cycle non-specific alkylating agent. Its primary physiological action is to cause DNA alkylation, damaging the cell's genetic material to block the machinery necessary for growth and reproduction. Lomustine is structurally distinct and highly lipid-soluble, a crucial property that allows it to effectively and readily cross the blood-brain barrier. This characteristic contributes to its suitability for managing certain malignancies within the central nervous system.

Composition and Physical Form of the Medication

Gleostine is a single-ingredient medicine supplied in the form of capsules, which is a solid dosage form taken orally. The capsule formulation contains the active ingredient Lomustine combined with inactive excipients, such as pharmaceutical fillers. The use of an oral delivery system is a significant practical feature for this type of nitrosourea, as it simplifies the administration process compared to related compounds that typically require intravenous infusion. Gleostine is currently the only brand-name Lomustine product available in the United States, replacing the original brand CeeNU.

Regulatory References

  1. Lomustine (CCNU) LiverTox

What side effects are possible with Gleostine?

Possible Side Effects and Safety Information

The safety profile of Gleostine (Lomustine) is primarily defined by the occurrence of documented adverse reactions classified by frequency and affected body systems, as stated in official regulatory labels.

Adverse Reaction Frequency
Very Common: Delayed myelosuppression (low white blood cell and platelet counts), nausea, and vomiting.
Common: Stomatitis (mouth sores), alopecia (hair loss), and anorexia.
Rare: Pulmonary fibrosis, optic atrophy, visual disturbances, and renal or hepatic toxicity.

Myelosuppression is the most frequent and serious toxicity, noted as delayed, dose-related, and cumulative. The lowest blood cell counts (nadir) typically occur four to six weeks following administration. Due to this delayed effect, blood counts are required to be monitored weekly for at least six weeks after each dose.

Serious Adverse Reactions and Time-Related Patterns

Documented serious adverse reactions include pulmonary toxicity, which may be fatal and is associated with cumulative doses generally exceeding 1100 mg/m^2, with an onset often six months or longer after therapy initiation. Long-term exposure is also associated with the risk of secondary malignancies, such as acute leukemia and myelodysplastic syndrome.

Population and Status Restrictions

Gleostine is officially contraindicated in individuals with severe, pre-existing bone marrow depression or known hypersensitivity to the drug or other nitrosoureas. Based on animal data, the medication is contraindicated during pregnancy due to the potential for fetal harm. Caution and monitoring are specified for patients with impaired renal function, reflecting the kidney's role in the drug's excretion and the risk of progressive nephrotoxicity.

Overdose and Emergency Response

Gleostine Overdose and When to Seek Help

The official regulatory profile for Gleostine (Lomustine) overdose centers on the severe and potentially fatal outcomes associated with overexposure. The most critical risk is delayed bone marrow suppression (myelosuppression), which is typically prolonged and leads to severe leukopenia and thrombocytopenia. These conditions carry the risk of life-threatening complications, including overwhelming infections and significant bleeding.

Acute, non-hematologic manifestations documented in regulatory sources include abdominal pain, diarrhea, vomiting, nausea, lethargy, and dizziness. Abnormal hepatic function has also been documented.

Emergency Action and Supportive Management

It is officially mandated to seek immediate medical attention for any suspected overdose. Furthermore, emergency services must be called immediately if the person has collapsed, had a seizure, has trouble breathing, or cannot be awakened. Treatment is strictly symptomatic and supportive, based on the patient's condition, because no specific antidote is known for Lomustine. Regulatory labeling describes supportive procedures such as immediate gastric lavage and appropriate post-overdose care, including infection prophylaxis and necessary blood product replacement.

Therapeutic Uses of Gleostine

Gleostine (Lomustine) is an established chemotherapy agent primarily used in situations involving certain distressing symptoms related to advanced cancers. It is commonly used to help manage specific, aggressive malignancies. The main therapeutic approach is used across domains where additional symptomatic support is needed for conditions presenting with systemic or localized discomfort, including aggressive tumors like recurrent glioblastoma multiforme (GBM) and relapsed Hodgkin's lymphoma.

By addressing the underlying malignancy, the medication provides support that helps ease the overall symptom burden in conditions marked by increased physiological stress. The approach is relevant for managing symptoms that interfere with daily comfort, such as neurological deficits caused by tumor pressure or systemic issues linked to advanced lymphoma. It is often applied in clinical settings that involve unstable symptom patterns, supporting patients during episodes of heightened discomfort.

Quick Fact: Managing Symptoms Linked to Organ-Specific Functional Stress This medication provides supportive relief when symptoms interfere with routine activities, and assists with managing symptoms related to increased neurological or muscular activity.

Regulatory References

  1. Official NIH DailyMed Drug Information

Eligibility and Restrictions for Use

Gleostine (lomustine) use is explicitly governed by official regulatory guidance that defines eligible populations and those for whom use is prohibited or restricted. The single formal contraindication is for individuals with a previous demonstrated hypersensitivity to lomustine or any of its components.

Populations for Whom Use is Restricted or Prohibited

Population Category Official Eligibility Status
Pregnancy Prohibited. The drug can cause fetal harm (Pregnancy Category D). Women of childbearing potential must use effective contraception during and after treatment.
Lactation Prohibited. Women must not breastfeed during treatment and for a specified period after the final dose.
Pulmonary Fibrosis Prohibited. Treatment must be permanently discontinued in patients who develop pulmonary fibrosis.
Pre-existing Pulmonary Impairment Restricted. Patients with a baseline Forced Vital Capacity (FVC) or Carbon Monoxide Diffusing Capacity (DLCO) below 70% of the predicted value are at increased risk and require special consideration.
Vaccines Contraindicated. Use with live attenuated vaccines is contraindicated.

Age and Eligibility

The medicine is formally indicated for use in adult and pediatric patients for its approved therapeutic uses, with dosage adjusted by body surface area (mg/m^2).

What should I know about interactions with other medicines?

The official regulatory profile for Gleostine (lomustine) defines several clinically significant drug-drug and population-specific interactions, which are classified based on the level of constraint required for their co-administration.

Contraindicated Combinations

Co-administration with Live Vaccines (including Yellow Fever, BCG, and Cholera Vaccine) is strictly prohibited. This is classified as a contraindicated combination due to the immunosuppressive effect of Lomustine, which significantly increases the risk of a severe systemic vaccine-associated infection.

Pharmacokinetic and Pharmacodynamic Interactions

The most commonly documented interactions fall into two categories:

  • Exposure-Altering Agents: Certain co-administered medicines modify the body's handling of Lomustine. Enzyme-Inducing Antiepileptic Drugs (e.g., Phenobarbital) may cause microsomal liver enzyme induction, accelerating clearance and potentially resulting in a reduced antitumour effect. Conversely, Enzyme-Inhibiting Drugs (e.g., Valproic Acid) are documented to impair metabolism, leading to increased toxicity.
  • Additive Toxicity: Concomitant use with other Cytostatic Agents or Radiation Therapy results in documented additive myelosuppression (increased bone marrow depression). Theophylline and Cimetidine are also noted to potentiate bone marrow toxicity.

Formal Regulatory Restrictions

Beyond drug interactions, the regulatory label contains two specific constraints:

  • Excipient Restriction: Due to the presence of wheat starch, the product must not be taken by patients with a documented wheat allergy.
  • Population Risk: Caution is formally noted for patients with impaired renal function, as the risk of toxic reactions may be greater due to the role of renal excretion in eliminating the drug and its metabolites.

No mandatory time-based administration separation rules for drug-drug combinations are explicitly documented in the official regulatory labeling.

Mechanism of Action

Genetic and Cellular Machinery Disruption

This domain covers the drug's direct chemical modification of cellular components, resulting in inhibited replication.

Gleostine functions primarily as an alkylating agent, which involves chemically modifying and damaging the DNA and RNA of the cell. The active compounds cause interstrand cross-links in the DNA helix, which physically prevents the DNA from separating and being copied or transcribed. This irreversible interference with the genetic material halts fundamental replication and transcription pathways, leading directly to the inhibition of cellular reproduction.

Blood-Brain Barrier Penetration and Mechanistic Limitations

This domain addresses the unique physical properties of the molecule that enable its distribution and the mechanisms of biological resistance that constrain its effect.

Lomustine is highly lipid-soluble, a structural property that allows it to easily bypass the Blood-Brain Barrier (BBB), allowing the cytotoxic mechanism to be delivered to cells within the Central Nervous System (CNS). However, the drug's mechanism faces a biological challenge: the MGMT enzyme acts as a specialized DNA repair system that can reverse the alkylation damage. When tumor cells express high levels of this enzyme, the drug's effect is diminished, limiting its ability to induce lethal damage and resulting in potential mechanism resistance.

Dosage and Administration Information

How to Use Gleostine (Lomustine) Capsules

Gleostine (lomustine) is an oral chemotherapy medication prescribed for use in cycles. The instructions for proper administration are strictly defined to ensure safety and effectiveness.


Administration and Dosage

Gleostine is supplied as hard capsules for oral administration. The total prescribed dose for a single cycle is typically composed of a combination of the available 5 mg, 10 mg, 40 mg, and 100 mg capsule strengths.

Administration Detail Official Instruction
Route of Administration Oral
Physical Handling Swallow capsules whole with water. Do not break, chew, or open the capsules.
Timing Relative to Meals May be taken on an empty stomach (e.g., at bedtime) to potentially reduce nausea and vomiting.

Dosing Schedule and Cycle Timing

Gleostine is administered as a single dose once per treatment cycle, with strict rules governing the waiting period before the next dose.

Cycle Requirement Official Instruction
Initial Single Dose 130 mg/m^2 (milligrams per square meter of body surface area).
Frequency Constraint The dose must not be repeated for a minimum of 6 weeks (42 days).
Dose Adjustment Subsequent doses must be modified or delayed based on the patient's nadir (lowest) blood cell counts following the previous administration.

All patients, including pediatric patients, are subject to this cyclic administration schedule and dose adjustment protocol. The proper use of Gleostine hinges on strictly following the single-dose rule and the minimum six-week interval between courses.

Recent Clinical Evidence

Gleostine: Recent Clinical Evidence

Evidence for use in Brain Tumors (Glioblastoma and Astrocytoma)

Research primarily focused on the use of Lomustine in adult patients whose high-grade brain tumors, such as Glioblastoma Multiforme (GBM) or Anaplastic Astrocytoma, had returned or progressed after initial treatment. This medication was evaluated in clinical trials, including Phase III Randomized Controlled Trials (RCTs), where it was observed in studies as monotherapy or in combination with newer agents. These studies monitored measurements of how long patients survived overall (OS) and the duration of the progression-free interval (PFS).

In these research settings, studies explored outcomes related to systemic or functional imbalance, such as tumor response rates. The research also investigated specific subgroups, such as those whose tumors carried a molecular marker known as MGMT methylation. The evidence level for this indication is broadly classified as Moderate. A limitation is that direct comparative evidence against a non-active control (such as placebo) is lacking in the current research landscape for recurrent disease.

Evidence for use in Relapsed Hodgkin's Lymphoma

Lomustine was studied for its role in managing Hodgkin's lymphoma that has relapsed or progressed following initial chemotherapy. The evidence base here is generally composed of older clinical investigations and systematic reviews, which often describe Lomustine as part of a multi-drug combination regimen used after the initial treatment has been completed. Studies monitored outcomes such as the overall Objective Response Rate (ORR), which measures tumor shrinkage. The certainty for this indication remains at a Moderate level. The primary limitation is that comparative evidence is lacking from contemporary, large-scale single-agent RCTs that meet today's standards.

The Overall Research Landscape and Uncertainty

Research has explored long-term outcomes, with some clinical trials observing survival for up to three to four years. However, data regarding sustained functional status in these populations are not fully established. Studies also included specific populations, such as pediatric patients for certain brain tumors. Nevertheless, data for certain groups remain insufficient, and subgroup findings are uncertain. Furthermore, in several studies, findings were mixed regarding the correlation between the measured progression-free interval and overall survival. This phenomenon indicates an area of uncertainty in the research.

Key Studies & References

  1. LOMUSTINE capsule drug information (Hodgkin's Lymphoma indication and safety overview)
  2. Lomustine - LiverTox: Clinical and Research Information on Drug Induced Liver Injury

Frequently Asked Questions (FAQ)

Common questions about Gleostine (FAQ)

Q: What is the main reason a doctor would prescribe Gleostine?

According to the official product information, Gleostine's FDA-approved indications are for the treatment of brain tumors, including primary and metastatic types. It is also approved for treating Hodgkin's lymphoma that has progressed after other chemotherapy treatments, often in combination with other agents.

Q: Do people ever use Gleostine for other types of cancer besides its main uses?

The FDA-approved uses for Gleostine are specifically limited to treating brain tumors and Hodgkin's lymphoma. Official regulatory bodies have not granted approval for other uses, meaning any other application is considered a non-approved indication.

Q: Are there any foods or drinks that are known to interact with Gleostine?

Official product information does not specify formal drug-food interactions for Gleostine. However, patients are often advised to take the medication on an empty stomach, such as at bedtime, because this may help minimize feelings of nausea and vomiting. This recommendation is related to managing a common side effect.

Q: Why is alcohol generally not recommended while taking Gleostine?

Official sources note that information regarding a specific interaction with alcohol is unknown. Due to the serious nature of this medication and its potential effects on organs, caution is generally exercised. Regulatory information often suggests caution or avoidance of alcohol use while undergoing treatment.

Q: Does Gleostine affect fertility in men or women?

The official label indicates that the drug can cause harm to a fetus, requiring women of reproductive potential to use contraception during and after treatment. As Gleostine is an alkylating agent—a class of drugs that damages genetic material—similar medications are often associated with effects on both male and female reproductive organs, and this may impact fertility.

Q: Do I need to change my lifestyle while taking Gleostine?

Regulatory documents highlight two key areas: infection risk and reproductive risk. The risk of infection due to myelosuppression means that precautions to minimize exposure to infections may be necessary. Furthermore, females of reproductive potential are required to use effective contraception due to the potential for the drug to cause fetal harm.

Q: Can Gleostine affect my ability to drive or operate machinery?

Official product information lists several neurological side effects that may impact physical and mental function. These reported adverse reactions include disorientation (confusion), lethargy (extreme tiredness), and visual disturbances. These effects may impact a person's ability to safely drive or operate heavy machinery.

Q: Does Gleostine affect my ability to think or concentrate?

Official product information notes that the drug can be associated with neurological adverse reactions. These effects include disorientation and lethargy (feeling extremely tired). Because of these potential effects, a person's ability to think clearly or concentrate may be impaired while on this medication.

Q: What are the official warnings or boxed warnings associated with Gleostine?

Gleostine carries a Boxed Warning in the US, which is the most serious level of warning required by the FDA. This warning primarily relates to bone marrow suppression (myelosuppression). Official documents describe this effect as delayed, cumulative, and potentially leading to fatal infections or bleeding.

Q: What are the signs that Gleostine might be affecting my blood counts?

The most common serious effect is low blood cell counts, which can manifest as physical symptoms. Official documents note that signs such as a fever, chills, sore throat, or unusual bleeding and bruising are reasons to seek medical advice. These symptoms can be indications that your white blood cell or platelet counts are low.

Q: What are the signs of a serious allergic reaction to Gleostine?

The official drug information contraindicates the use of Gleostine in individuals with a known hypersensitivity (allergic reaction) to the drug itself. Allergic reactions typically involve symptoms such as a rash, generalized swelling, or difficulty breathing, which are considered medical emergencies.

Q: What should I do if my side effects from Gleostine become severe?

Regulatory guidance specifies that prompt contact with a physician is necessary if any severe reactions occur. Official guidance lists symptoms such as fever, chills, sore throat, unusual bleeding, shortness of breath, a dry cough, or swelling of the feet or lower legs as reasons to seek medical advice immediately.

Q: Can Gleostine be prescribed by a general practitioner, or only a specialist?

Due to the drug's cytotoxic nature, complex dosing, and need for specialized monitoring, official health policies often require that it be prescribed by, or in consultation with, a medical specialist such as an oncologist or hematologist. This ensures appropriate use and management of the treatment.

Q: Is there a maximum number of times someone can take Gleostine?

Regulatory information associates the risk of developing pulmonary toxicity (lung damage) with the total amount of medication received over time. This risk is generally linked to cumulative doses greater than 1100 mg/m^2 (milligrams per square meter of body surface area). This cumulative dose threshold is a key factor in determining the overall duration of therapy.

Q: Are there different restrictions for who can use Gleostine depending on the country?

Official regulatory requirements, such as those from the FDA (US) and the EMA (Europe), define eligibility and restrictions, and these can vary slightly across international bodies. For instance, some countries may add specific constraints, such as the severity of pre-existing low blood cell counts (leukopenia or thrombocytopenia), to the list of contraindications.

How should Gleostine be stored and disposed of?

Gleostine (Lomustine) Storage and Disposal

Storage of Gleostine capsules requires maintaining a controlled room temperature between 15 C and 30 C (59 F and 86 F). The medication must be kept in the original, well-closed container and protected from light and freezing to maintain stability. A crucial regulatory requirement is that Gleostine must be stored out of the reach of children.


Handling and Disposal

As a cytotoxic drug, special handling rules apply. The capsules must not be broken, crushed, or opened. Handlers must wear impervious gloves. Patients should ask their healthcare provider or pharmacist for instructions on disposing of unused or expired capsules. The product must be managed according to local cytotoxic waste procedures and not disposed of in household trash or down a drain.

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

Available in countries:

Equivalent of Gleostine found in:

A-Z Index: