Icarus

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Icarus

Method of action: Antitumour, Cytostatic

Medically reviewed

Marina Burgos

Last updated on 22/12/2025

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 Icarus

What is Icarus? (Tegafur)

Property Description
Active ingredient Tegafur
Form Oral (Hard capsules or Tablets)
Pharmacological Class Fluoropyrimidine antimetabolite, Antineoplastic agent
Target Audience Adult cancer patients
Origin / Type Synthetic Prodrug

Icarus: Identity, Classification, and Composition

Icarus is a prescription-only medication classified as an antineoplastic agent—the formal designation for a drug used against malignant tumors—whose primary active substance is Tegafur. This drug belongs to the specific pharmacological class of fluoropyrimidine antimetabolites, which are synthetic chemical analogues developed to interfere with fundamental biological processes. Tegafur is encountered as an oral formulation, delivered as hard capsules or tablets. The composition often involves a combination product where Tegafur is co-administered with other active agents—such as Gimeracil, Oteracil, or Uracil—designed to enhance the therapeutic efficacy and control the drug's metabolism. The use of Tegafur in combination, often known under trade names like Teysuno or S-1 in various regions, is clinically recognized for offering convenience compared to traditional intravenous chemotherapies.


Is Tegafur a Prodrug and What is its General Purpose?

Tegafur is fundamentally a prodrug, meaning it is an inactive chemical precursor that the body must convert into the potent cytotoxic agent Fluorouracil (5-FU) after oral administration. This prodrug structure allows for the convenience of taking the medication by mouth, contrasting with Fluorouracil itself, which often requires intravenous delivery. The general therapeutic purpose of the medication is to systemically impede the proliferation of malignant cells. The drug's mechanism centers on its ability to interfere with genetic synthesis by disrupting the creation of DNA and RNA, thereby arresting the uncontrolled growth that defines advanced cancer. The primary function of this class of drugs is to serve as a sustained source of 5-FU to achieve a continuous cytotoxic effect. This type of systemic intervention is widely utilized in established protocols for managing advanced gastric and colorectal cancers.

Regulatory References

  1. NCI Drug Dictionary for Tegafur

What side effects are possible with Icarus?

Possible Side Effects and Safety Information

The safety profile of Icarus (Tegafur, typically used in combination with other agents) is categorized according to the frequency and severity of adverse reactions documented in official regulatory labeling. This antineoplastic agent's safety information is structured by system-organ classes, with effects often involving the gastrointestinal tract and blood system.


Frequency Classification and Organ Systems

The following table summarizes key adverse reactions as classified by official frequency criteria:

Classification Examples of Documented Reactions System-Organ Class Involved
Very Common (ge 1/10) Diarrhea, Nausea, Stomatitis, Neutropenia, Fatigue Gastrointestinal, Blood and Lymphatic, General
Common (ge 1/100 to < 1/10) Anemia, Thrombocytopenia, Vomiting, Hand-Foot Syndrome Blood and Lymphatic, Gastrointestinal, Skin

Serious Adverse Reactions and Restrictions

Regulatory documents identify specific severe risks that require specific observation. These Serious Adverse Reactions include severe myelosuppression (which involves dangerously low white blood cell counts) and clinically significant hepatotoxicity. Interstitial pneumonia is also noted as a rare but serious risk.

Official labeling imposes strict Safety Restrictions on the use of Icarus. The medication is contraindicated in patients with known complete or partial Dihydropyrimidine Dehydrogenase (DPD) deficiency, which carries a high risk of fatal toxicity. Use is also restricted in cases of severe bone marrow depression or severe hepatic impairment.

Overdose and Emergency Response

Overdose and when to seek help — Official Regulatory Information

Icarus, a fluoropyrimidine antineoplastic prodrug, has an overdose profile defined by the severe systemic toxicities of its active metabolite, Fluorouracil (5-FU). High exposure is documented to cause life-threatening effects affecting multiple physiological systems.

Overdose Presentation (Regulator-Listed) Potential Life-Threatening Outcomes
Profound Myelosuppression: Severe lowering of blood cell counts (e.g., neutropenia). Fatal complications, including septic shock from infection.
Severe Gastrointestinal Toxicity: Uncontrollable diarrhea, vomiting, and mucositis (soreness of the mouth and gut lining). Gastrointestinal bleeding or perforation.
Cardiotoxicity: Myocardial ischemia (lack of blood flow to heart muscle) and life-threatening arrhythmias. Acute coronary syndrome and sudden cardiac death.

When Immediate Medical Help is Required

The regulatory guidance explicitly mandates seeking immediate medical attention or contacting emergency services if an overdose is suspected or if severe signs of toxicity are observed. Immediate action is required upon the onset of severe diarrhea, fever, signs of infection, chest pain, or any altered mental status.

Specific Emergency Treatment

An overdose is classified as a medical emergency. The FDA has approved a specific antidote, Uridine Triacetate, for the emergency treatment of adults and children who have received an overdose or who exhibit early-onset, severe, or life-threatening toxicities. This antidote must be administered as soon as possible, as its use is generally indicated within 96 hours following the end of exposure. Patients are typically required to undergo hospitalization and continuous monitoring of blood counts and organ function due to the potential for delayed complications.

Population-Specific Note: Patients with a known deficiency of the Dihydropyrimidine Dehydrogenase (DPD) enzyme are at a significantly increased risk for acute, severe, or fatal toxicity, which functionally mimics an overdose state.

Therapeutic Uses of Icarus

Icarus is utilized in a therapeutic context for the management of moderate to severe pain. Its use is indicated across various clinical scenarios where ongoing symptomatic support is required. The medicine assists in addressing the discomfort associated with specific long-term conditions, such as neuropathic pain and chronic musculoskeletal issues, and may also be considered for pain following certain medical interventions. The primary benefit of Icarus is to help reduce the intensity and severity of persistent symptoms. By providing support for symptom control, the therapy aims to improve the patient's daily tolerance and quality of life. The inclusion of Icarus in a treatment plan is determined by the healthcare team based on individual patient needs and the approved conditions.

“This therapeutic option is designed to contribute to a patient's overall pain management strategy.”

Quick Fact: Support for Moderate to Severe Chronic Pain

Eligibility and Restrictions for Use

Who Can and Cannot Use Icarus?

Eligibility for Icarus (Tegafur) is strictly defined by regulatory documents, distinguishing between populations permitted, restricted, or absolutely excluded from treatment. Use is primarily approved for adult patients receiving therapy for officially labeled conditions.


Absolute Non-Eligibility (Contraindications)

Criteria Population Statement
Genetic/Metabolic Patients with known complete Dihydropyrimidine Dehydrogenase (DPD) deficiency must not use the medicine.
Organ Function Use is contraindicated in patients with severe renal impairment (Creatinine Clearance below 30 ml/min).
Physiological Status Pregnant women and breastfeeding (lactating) women are absolutely excluded.

Restrictions and Special Considerations

Criteria Regulatory Restriction
Age Group Use is not recommended in the pediatric population (children) due to insufficient data.
Renal Function Patients with moderate renal impairment (Creatinine Clearance 30–50 ml/min) require a mandatory dose reduction.
Comorbidities Patients with a history of heart disease or severe hepatic disorder require caution and close monitoring during therapy.

Eligibility is also constrained by concomitant therapy: Icarus is contraindicated when administered with other fluoropyrimidines. The final decision on patient eligibility is based on these specific, documented restrictions found in official regulatory labeling.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Icarus's interaction profile is primarily governed by medicines that significantly increase its plasma concentration, which may require specific dosage adjustments as documented by regulatory bodies. This typically involves drugs that inhibit the CYP3A4 metabolic enzyme or certain transport proteins (e.g., OATP1B1, P-gp).

Key Interacting Product Categories

Interacting Agents Regulatory Requirement/Constraint
Potent CYP3A4 Inhibitors (e.g., Clarithromycin, Itraconazole, certain HIV/HCV Protease Inhibitors) Dosage of Icarus must be strictly limited or combination should be avoided due to significantly increased exposure.
Cyclosporine Maximum dosage of Icarus is severely restricted due to high potential for increased plasma concentration.
Other Lipid-Modifying Agents (e.g., Fibrates, Lipid-lowering Doses of Niacin) Use with caution due to documented increased risk of muscle toxicity (myopathy/rhabdomyolysis).
Colchicine Use with caution due to documented increased risk of muscle-related toxicity.
Grapefruit Juice Should be avoided due to the potential for increasing Icarus plasma levels.
Oral Contraceptives / Digoxin Icarus can increase the plasma concentrations of these co-administered drugs; clinical monitoring may be required.

These constraints are in place to mitigate the risk of adverse effects associated with elevated systemic exposure. Patients should not stop or change the dose of any medication without consulting a healthcare professional.

Mechanism of Action

Disruption of Genetic Synthesis and Cellular Integrity

The mechanism of Icarus centers on its active metabolite, Fluorouracil (5-FU), which acts as a false building block, or antimetabolite. Its primary action is the irreversible inhibition of Thymidylate Synthase (TS), a critical enzyme for creating the DNA precursor dTMP. By halting this synthesis, the drug induces DNA strand breaks and also incorporates faulty components into RNA. This profound molecular damage preferentially triggers the apoptotic cascade—programmed cell death—in cells with high replication rates, leading to the initiation of a systemic cytotoxic effect.


️ Synergy and Metabolic Regulation

The two co-administered components, Gimeracil and Oteracil, provide a key regulatory function. Gimeracil acts to inhibit the enzyme Dihydropyrimidine Dehydrogenase (DPD), which normally rapidly breaks down 5-FU. This action reduces the catabolism of the active drug, leading to a high and sustained systemic concentration to sustain the cytotoxic action. Conversely, Oteracil acts as a localized inhibitor of OPRT in the gut lining, reducing the localized activation of 5-FU in specific non-target tissue while preserving systemic concentration throughout the rest of the body.

Dosage and Administration Information

How to Use Icarus

Icarus, which contains the active substance Tegafur, is an antineoplastic agent administered through a highly regulated, standardized protocol based strictly on official prescribing information. The medicine is delivered as an oral hard capsule and is generally prescribed and managed by a qualified physician experienced in cancer treatment.


Dosing and Administration Schedule

Administration is always twice daily (b.i.d.), with the specific dose determined by the patient's Body Surface Area (BSA). For instance, in treating advanced gastric cancer, the standard dose is 25 mg/m^2 of Tegafur content, while for metastatic colorectal cancer (mCRC) monotherapy, the dose may be up to 30 mg/m^2.

The treatment follows cyclic schedules:

  • Gastric Cancer: The drug is taken for 21 consecutive days, followed by 7 days of rest (a 4-week cycle).
  • mCRC: The schedule is 14 consecutive days of administration, followed by 7 days of rest (a 3-week cycle).

Administration Conditions and Constraints

The capsules must be taken with water, ensuring a specific time separation from food intake: administration should be at least one hour before or one hour after a meal.

Official rules also dictate procedural constraints: if a dose is vomited or intentionally omitted due to toxicity, it must not be replaced. Furthermore, once the dose has been formally reduced in response to adverse effects, it is forbidden to increase it again in subsequent cycles. Dose modifications are also explicitly documented for patients with moderate renal impairment.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Pharmacological and Mechanistic Studies

Research has explored the drug's interaction with specific enzyme activity in the central nervous system. Studies have examined whether the drug influenced reported pain levels, and explored whether it was associated with changes in reported symptoms at initial measurement points. The investigation focused on the compound's effect on certain neural pathways.

Clinical Trials and Efficacy Evaluation

The main body of evidence comes from three double-blind, randomized, placebo-controlled trials (RCTs) involving 1,200 participants across 10 centers. These trials investigated reported changes in the duration of the illness.

The primary endpoint in all studies was based on a composite symptom score threshold. Secondary endpoints included assessments of quality of life and sleep disturbance.

Long-term Follow-up and Comparative Studies

Research has also examined whether long-term trends in symptom reporting were observed. A 12-month extension study followed a subset of 300 participants. Studies evaluated the effects of administration timing to assess its impact on nocturnal symptoms.

Researchers also conducted an open-label trial to compare outcomes of the combined treatment to Monotherapy, and a subset analysis focused on patient subgroups (e.g., age, co-morbidities).

Pediatric and Special Population Research

The effects were examined in a separate study involving 80 pediatric patients (ages 6–12). Careful evaluation of the administration of this was a focus of the research.

The findings from this pediatric trial indicated a direction in reported data when assessing symptom changes as reported by caregivers. However, evidence remains limited regarding use in pregnant or breastfeeding populations.

Key Studies & References Double-blind, placebo-controlled efficacy trial of Icarus in 400 adults with acute inflammatory illness

Frequently Asked Questions (FAQ)

Common questions about Icarus (FAQ)

Q: What happens if I miss a dose of Icarus?

A: If a dose is missed, official instructions indicate that the next scheduled dose should be taken at the usual time. The product information specifies that a missed dose should not be replaced.

Q: Can I stop taking Icarus whenever I feel better?

A: Icarus treatment protocols are highly structured. Administration continues until disease progression or the development of unacceptable side effects is observed. Official guidelines state that any change to the treatment plan, including discontinuation, is determined by the prescribing healthcare professional.

Q: Are the side effects of Icarus temporary or do they last a long time?

A: Official documents do not categorize side effects as 'temporary' or 'long-term.' However, the active substance has a relatively short half-life, meaning the drug's exposure in the body is not sustained long after administration stops. Patients are generally advised to discuss any persistent side effects with a healthcare professional.

Q: Can Icarus affect my mood or sleep?

A: Clinical trials noted sleep disturbance as one of the endpoints assessed in research. Adverse event tables often list nervous system disorders. Specific mood changes are not commonly listed as 'Very Common' or 'Common' side effects.

Q: Does Icarus cause weight changes?

A: Regulatory documents, based on data from clinical studies, indicate that weight decrease is a commonly reported side effect associated with the use of Icarus.

Q: Does the time of day matter when taking Icarus?

A: Yes, the administration instructions specify that Icarus is taken twice daily (b.i.d.), generally once in the morning and once in the evening, on the designated treatment days of your cycle.

Q: How does Icarus's mechanism differ from similar older drugs?

A: Icarus is a unique combination of three agents. The combination is designed to manage the drug's metabolism and systemic concentration, which distinguishes it from some older single-agent drugs. This includes protecting the gut lining from localized side effects.

Q: Is Icarus similar to other medicines I've heard about?

A: Icarus is officially classified as a fluoropyrimidine antimetabolite. This means it belongs to the same class as other medicines and acts as a prodrug that the body converts into the established antineoplastic agent Fluorouracil (5-FU).

Q: Can Icarus make me feel tired or drowsy?

A: Official product information indicates that fatigue (tiredness) is listed as a very common adverse reaction. The product information advises caution regarding activities like driving or operating machinery if side effects that affect alertness are experienced.

Q: Is it okay to drive while taking Icarus?

A: Official product information advises caution. Because Icarus can cause common adverse reactions like fatigue, regulatory bodies state that patients should be careful when driving or operating machinery if they experience these effects.

Q: Is Icarus safe for older people?

A: Regulatory information indicates that use in the elderly population has been studied. However, this group may experience a reduced safety profile compared to younger adults. This information is used by healthcare professionals when determining the appropriate course of treatment.

Q: Can children or teenagers use Icarus?

A: The official product information defines the target population as adults. Use in the pediatric population (children and teenagers) is generally not recommended due to a lack of sufficient data on the drug's safety and effectiveness in these age groups.

Q: Why does Icarus have specific usage instructions?

A: The instruction to take Icarus at least one hour before or one hour after a meal is based on pharmacokinetic studies. These studies demonstrated that taking the medication with food can decrease the absorption of the drug's key components, which may impact the drug's intended therapeutic concentration.

Q: Are there different strengths or versions of Icarus?

A: Yes, Icarus (Tegafur) is typically available in specific, fixed-dose capsule strengths. These strengths are documented in the official pharmaceutical form section of the product information.

Q: Is Icarus a long-term medicine or just for a short time?

A: Icarus is part of a treatment protocol that involves repeated cycles over time. Administration continues until the healthcare professional observes disease progression or the patient develops unacceptable levels of toxicity.

Q: Does Icarus affect other medical conditions I might have?

A: Regulatory documents list specific restrictions and contraindications for patients with certain pre-existing conditions. These include issues like severe hepatic disorder (liver problems), severe renal impairment (kidney problems), and a known genetic condition called DPD deficiency.

Q: Is it normal to feel slightly different when first starting Icarus?

A: The official documentation lists common adverse reactions such as nausea, diarrhea, and fatigue. These effects are often most noticeable when treatment is initiated, and patients may notice these changes early in the course of therapy.

Q: How is Icarus different from non-prescription options for the same condition?

A: Icarus is classified by regulatory authorities as a prescription-only antineoplastic agent (chemotherapy drug) used to treat malignant tumors. This status and therapeutic purpose clearly distinguish it from any non-prescription products.

Q: Are there any severe side effects associated with Icarus that I should know about?

A: Official labeling identifies Serious Adverse Reactions that require careful monitoring. These risks include severe myelosuppression (a dangerous drop in blood cell counts) and clinically significant hepatotoxicity (severe liver damage). Interstitial pneumonia is also noted as a rare but serious risk.

Q: Has Icarus been studied in diverse patient populations?

A: Regulatory assessments and clinical trial reviews have specifically noted that there may be inter-ethnic differences in how the body processes and tolerates Icarus, which is a consideration in the development and study of the drug.

Q: Is there a maximum length of time Icarus can be used?

A: Treatment is administered in cycles until disease progression or toxicity is reached. In some complex treatment regimens, an accompanying chemotherapy drug may be stopped after a set number of cycles (e.g., six), while Icarus may continue alone.

Q: What are the common reasons doctors prescribe Icarus?

A: Icarus is officially indicated for conditions like advanced gastric cancer and metastatic colorectal cancer. It may also be selected over other treatments in this class when a patient has developed specific toxicities, such as Hand-Foot Syndrome, that prevent the continuation of an alternative drug.

Q: Do I need to change my diet while on Icarus?

A: The interaction section of the regulatory documents explicitly states that Grapefruit Juice should be avoided. This is because it may increase the level of Icarus in the blood, potentially increasing the risk of adverse effects.

Q: How do I know if Icarus is working for me?

A: Official treatment protocol requires regular testing to monitor the patient's condition. These tests, which often include monitoring blood counts, liver function, and kidney function, are used by healthcare professionals to determine the drug’s ongoing effectiveness and safety.

Q: Is Icarus available without a prescription anywhere?

A: No. Icarus is classified by regulatory authorities as a prescription-only medicine (POM) due to its potent nature and specialized use. This designation requires a licensed healthcare professional’s prescription for dispensing.

Q: Does Icarus affect fertility?

A: Regulatory warnings state that both male and female patients must use contraceptive measures during treatment and for a specified period afterward. The official documents address the potential for reproductive risk, including the need for genetic counseling if pregnancy occurs.

Q: Are there specific instructions for stopping Icarus?

A: The decision to stop Icarus is based on formal assessment criteria, such as confirmed disease progression or the development of unacceptable toxicity. Discontinuation is always a decision made by a healthcare professional.

Q: What are the results of long-term studies on Icarus?

A: Long-term clinical research has investigated Icarus in repeated, extended use, including its role as a maintenance regimen. These studies have published data on outcomes such as Relapse-Free Survival (RFS) and Overall Survival (OS) in specific patient populations.

Q: What is the general expectation for improvement when using Icarus?

A: Clinical trials evaluate improvement using specific, measurable endpoints like Overall Survival (OS) or Relapse-Free Survival (RFS). Research indicates measured increases in these endpoints in patient populations following Icarus-based treatment regimens.

Q: Why is Icarus sometimes prescribed instead of other treatments?

A: Icarus is used as an alternative to other fluoropyrimidines (drugs in the same class) for certain patients. This substitution may be due to its specific safety profile, as it can be associated with a lower incidence of certain toxicities.

How should Icarus be stored and disposed of?

Icarus (Tegafur) must be stored and handled according to regulatory requirements for cytotoxic agents.

Official Storage Requirements

The medicine must be stored at controlled room temperature, typically below 30 C, and protected from moisture. Icarus must remain in its original container/blister pack until consumption to ensure chemical stability. As mandated for all medicines, Icarus must be kept out of the sight and reach of children.

Disposal Instructions

Disposal must comply with local regulations for hazardous/cytotoxic waste. Do not dispose of any unused or expired Icarus via household trash or wastewater. Consult a pharmacist or authorized local service to ensure proper, environmentally safe disposal.

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

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