Erlonat is a cancer medicine that interferes with the growth of cancer cells and slows their spread in the body.
Erlonat is used to treat non-small cell lung cancer or pancreatic cancer that has spread to other parts of the body (metastatic).
Erlonat is usually given after other cancer medicines have been tried without success.
Erlonat may also be used for purposes not listed in this medication guide.
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
Non-Small Cell Lung Cancer (NSCLC)
Erlonat is indicated for:
The first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
The maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer whose disease has not progressed after four cycles of platinum-based first-line chemotherapy.
The treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen.
Limitations of use:
Erlonat is not recommended for use in combination with platinum-based chemotherapy.
Safety and efficacy of Erlonat have not been evaluated as first-line treatment in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution.
Erlonat in combination with gemcitabine is indicated for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer.
How should I use Erlonat?
Use Erlonat as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Take Erlonat by mouth with a glass of water on an empty stomach at least 1 hour before or 2 hours after eating.
Wash your hands immediately after taking Erlonat.
Eating grapefruit or drinking grapefruit juice while you are taking Erlonat may increase the amount of Erlonat in your blood, which may increase your risk of serious side effects. Talk with your doctor before including grapefruit or grapefruit juice in your diet.
Take Erlonat on a regular schedule to get the most benefit from it. Taking Erlonat at the same time each day will help you to remember to take it.
If you take an H receptor antagonist (eg, ranitidine) or an antacid, talk with your doctor or pharmacist about how to take these medicines together.
If you miss a dose of Erlonat, contact your doctor right away.
Ask your health care provider any questions you may have about how to use Erlonat.
Uses of Erlonat in details
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
Erlonat is used to treat lung and pancreatic cancer. It works by slowing or stopping the growth of cancer cells.
How to use Erlonat
Take this medication by mouth on an empty stomach (at least 1 hour before or 2 hours after a meal) as directed by your doctor, usually once daily.
The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Medications that lower stomach acid (such as antacids, H2 blockers including ranitidine) may prevent Erlonat from working. Ask your doctor or pharmacist how to use these medications safely with Erlonat.
Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.
Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.
Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.
Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.
Erlonat hydrochloride (trade name Erlonat, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, Erlonat specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlonat has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that Erlonat may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.
Dosage:Non-Small Cell Lung Cancer: EGFR mutation testing should be performed prior to initiation of Erlonat therapy in chemo-naive patients with advanced or metastatic NSCLC.
The recommended daily dose of Erlonat is 150 mg taken at least one hour before or two hours after the ingestion of food.
Pancreatic Cancer:The recommended daily dose of Erlonat is 100 mg taken at least one hour before or two hours after the ingestion of food, in combination with gemcitabine.
Special Dosage Instructions: Concomitant use of CYP 3A4 substrates and modulators may require dose adjustment.
When dose adjustment is necessary, it is recommended to reduce in 50 mg steps.
Hepatic Impairment:Erlonat is eliminated by hepatic metabolism and biliary excretion. Although Erlonat exposure was similar in patients with moderately impaired hepatic function (Child-Pugh score 7-9) compared with patients with adequate hepatic function, caution should be used when administering Erlonat to patients with hepatic impairment.
Dose reduction or interruption of Erlonat should be considered if severe adverse reactions occur. Safety and efficacy have not been studied in patients with severe hepatic impairment.
Renal Impairment: The safety and efficacy of Erlonat has not been studied in patients with renal impairment.
Pediatric Use: The safety and efficacy of Erlonat has not been studied in patients under the age of 18 years.
Smokers: Cigarette smoking has been shown to reduce Erlonat exposure by 50-60%.
The maximum tolerated dose of Erlonat in NSCLC patients who currently smoke cigarettes was 300 mg. Efficacy and long term safety of a dose higher than the recommended starting doses have not been established in patients who continue to smoke cigarettes.
Erlonat is metabolized in the liver by the hepatic cytochromes in humans, primarily CYP3A4 and to a lesser extent by CYP1A2 and the pulmonary isoform CYP1A1. Potential interactions may occur with drugs which are metabolized by, or are inhibitors or inducers of these enzymes.
Potent inhibitors of CYP3A4 activity decrease Erlonat metabolism and increase Erlonat plasma concentrations. Inhibition of CYP3A4 metabolism by ketoconazole (200 mg orally twice daily for 5 days) resulted in increased exposure to Erlonat (86% in median Erlonat exposure AUC) and a 69% increase in maximum plasma concentration (Cmax) when compared to Erlonat alone. When Erlonat was co-administered with ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlonat exposure (AUC) and Cmax increased by 39% and 17%, respectively. Therefore, caution should be used when administering Erlonat with potent CYP3A4 or combined CYP3A4/CYP1A2 inhibitors. In these situations, the dose of Erlonat should be reduced if toxicity is observed.
Potent inducers of CYP3A4 activity increase Erlonat metabolism and significantly decrease Erlonat plasma concentrations. Induction of CYP3A4 metabolism by rifampicin (600 mg orally everday for 7 days) resulted in a 69% decrease in the median Erlonat AUC, following Erlonat 150 mg, as compared to Erlonat alone.
Pre-treatment and co-administration of rifampicin with a single Erlonat 450 mg resulted in a mean Erlonat exposure (AUC) of 57.5% of that after a single 150-mg Erlonat dose in the absence of rifampicin treatment. Alternative treatments lacking potent CYP3A4 inducing activity should be considered when possible. For patients who require concomitant treatment with Erlonat and a potent CYP3A4 inducer eg, rifampicin, an increase in dose to 300 mg should be considered while their safety is closely monitored and if well tolerated for >2 weeks, further increase to 450 mg could be considered with close safety monitoring. Higher doses have not been studied in this setting.
Pre-treatment or co-administration of Erlonat did not alter the clearance of the prototypical CYP3A4 substrates midazolam and erythromycin. Significant interactions with the clearance of other CYP3A4 substrates are therefore unlikely.
Oral availability of midazolam did appear to decrease by up to 24%, which was however not attributed to effects on CYP3A4 activity.
The solubility of Erlonat is pH dependent. Erlonat solubility decreases as pH increases. Drugs that alter the pH of the upper gastrointestinal (GI) tract may alter the solubility of Erlonat and hence its bioavailability. Co-administration of Erlonat with omeprazole, a proton pump inhibitor, decreased the Erlonat exposure (AUC) and Cmax by 46% and 61%, respectively. There was no change to Tmax or half-life (t½). Concomitant administration of Erlonat with ranitidine 300 mg, an H2-receptor antagonist, decreased Erlonat exposure (AUC) and Cmax by 33% and 54%, respectively. Therefore, co-administration of drugs reducing gastric acid production with Erlonat should be avoided where possible. Increasing the dose of Erlonat when co-administered with such agents is not likely to compensate for this loss of exposure. However, when Erlonat was dosed in a staggered manner 2 hrs before or 10 hrs after ranitidine 150 mg twice daily, Erlonat exposure (AUC) and Cmax decreased only by 15% and 17%, respectively. If patients need to be treated with such drugs, then an H2-receptor antagonist eg, ranitidine should be considered and used in a staggered manner. Erlonat must be taken at least 2 hrs before or 10 hrs after the H2-receptor antagonist dosing.
Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased international normalized ratio (INR) and bleeding events, which in some cases were fatal have been reported in patients receiving Erlonat. Patients taking coumarin-derived anticoagulants should be monitored regularly for any changes in prothrombin time or INR.
The combination of Erlonat and a statin may increase the potential for statin-induced myopathy, including rhabdomyolysis, which was observed rarely.
Smokers should be advised to stop smoking as cigarette smoking, which is known to induce CYP1A1 and CYP1A2, has been shown to reduce Erlonat exposure by 50-60%.
In a phase Ib study, there were no significant effects of gemcitabine on the pharmacokinetics of Erlonat nor were there significant effects of Erlonat on the pharmacokinetics of gemcitabine.
Non-Small Cell Lung Cancer (Erlonat Administered as Single Agent in Study BR.21): In 1 randomized double-blind study BR.21 conducted in 17 countries, 731 patients with locally advanced or metastatic NSCLC after failure of at least 1 prior chemotherapy regimen were randomized 2:1 to receive Erlonat 150 mg or placebo. Study drug was taken orally once daily until disease progression or unacceptable toxicity.
Rash (75%) and diarrhea (54%) were the most frequent adverse events regardless of causality. Most were grade 1 or grade 2 in severity and manageable without intervention. Grade 3/4 rash and diarrhea occurred in 9% and 6%, respectively, in patients treated with Erlonat and each resulted in study discontinuation in 1% of patients. Dose reduction for rash and diarrhea was needed in 6% and 1% of patients, respectively. In study BR.21 the median time to onset of rash was 8 days and the median time to onset of diarrhea was 12 days.
Adverse events occurring more frequently (≥3%) in patients treated with Erlonat than in the placebo arm in the pivotal study BR.21 and in at least 10% of patients in the Erlonat arm, are summarized by National Cancer Institute-Common Toxicity Criteria (NCI-CTC) grade in Table 3. Listed events are assessed by the sponsor as being adverse drug reactions attributed to Erlonat therapy.
Pancreatic Cancer (Erlonat Administered concomittantly with Gemcitabine in Study PA.3): The most frequent adverse reactions in pivotal study PA.3 in pancreatic cancer patients receiving Erlonat 100 mg plus gemcitabine were fatigue, rash and diarrhea. In the Erlonat plus gemcitabine arm, Grade 3/4 rash and diarrhea were each reported in 5% of patients. The median time to onset of rash and diarrhea was 10 and 15 days, respectively. Rash and diarrhea each resulted in dose reductions in 2% of patients and resulted in study discontinuation in up to 1% of patients receiving Erlonat plus gemcitabine.
The Erlonat 150 mg plus gemcitabine cohort (23 patients) was associated with a higher rate of certain class-specific adverse reactions including rash and required more frequent dose reduction or interruption.
Adverse events occurring more frequently (≥3%) in Erlonat 100 mg plus gemcitabine-treated patients than in the placebo plus gemcitabine group in the pivotal study PA.3 and in at least 10% of patients in the Erlonat 100 mg plus gemcitabine group, are summarized by National Cancer Institute-Common Toxicity Criteria (NCI-CTC) Grade in Table 4. Listed events are assessed by the sponsor as being adverse drug reactions attributed to Erlonat therapy.
Other Observations (Based on Data from All Clinical Studies): Safety evaluation of Erlonat is based on the data from >800 patients treated with at least one Erlonat 150 mg monotherapy and >300 patients who received Erlonat 100 mg or 150 mg in combination with gemcitabine.
The following adverse reactions have been observed in patients who received Erlonat 150 mg as monotherapy or 100 mg or 150 mg in combination with gemcitabine.
The following terms are used to rank the adverse reactions by frequency: Very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10,000, <1/1000); very rare (<1/10,000) including isolated reports.
Very common adverse reactions (ADRs) are presented in Tables 3 and 4, ADRs in other frequency categories are summarized as follows.
Gastrointestinal Disorders: Gastrointestinal perforations have been reported uncommonly (<1% of patients) with Erlonat treatment, in some cases with a fatal outcome.
Cases of gastrointestinal bleeding have been reported commonly (including some fatalities), some associated with concomitant warfarin administration, and some with concomitant NSAIDs.
Liver function test abnormalities (including raised ALT, AST, bilirubin) have been observed commonly in clinical trials of Erlonat. In study PA.3, these occurred very commonly. They were mainly mild or moderate in severity, transient in nature or associated with liver metastases. Rare cases of hepatic failure (including fatalities) have been reported during use of Erlonat. Confounding factors have included preexisting liver disease or concomitant hepatotoxic medications.
Eye Disorders: Corneal ulcerations or perforations have been reported very rarely in patients receiving Erlonat treatment. Keratitis and conjunctivitis have been reported commonly with Erlonat.
Abnormal eyelash growth, including in-growing eyelashes, excessive growth and thickening of the eyelashes have been reported.
Respiratory, Thoracic and Mediastinal Disorders: There have been uncommon reports of serious ILD-like events, (including fatalities), in patients receiving Erlonat for treatment of NSCLC and other advanced solid tumours. Cases of epistaxis have also been reported commonly in both the NSCLC and the pancreatic cancer trials.
Skin and Subcutaneous Tissue Disorders: Rash has been reported very commonly in patients receiving Erlonat and in general, manifests as a mild or moderate erythematous and papulopustular rash, which may occur or worsen in sun-exposed areas. For patients who are exposed to sun, protective clothing and/or use of sun screen (eg, mineral-containing) may be advisable. Acne, dermatitis acneiform and folliculitis have been observed commonly, most of these events were mild or moderate and non-serious. Skin fissures, mostly non-serious, were reported commonly and in the majority of cases were associated with rash and dry skin. Other mild skin reactions eg, hyperpigmentation have been observed uncommonly (<1% of patients).
Bullous, blistering and exfoliative skin conditions have been reported, including very rare cases suggestive of Stevens-Johnson syndrome/toxic epidermal necrolysis, which in some cases were fatal.
Hair and nail changes, mostly non-serious, were reported in clinical trials, eg, paronychia was reported commonly and hirsutism, eyelash/eyebrow changes and brittle and loose nails were reported uncommonly.
Post-Marketing: Skin and Subcutaneous Tissue Disorders:
Hair and nail changes, mostly non-serious, were reported uncommonly from post-marketing surveillance eg, hirsutism, eyelash/eyebrow changes, paronychia and brittle and loose nails.
Cases of uveitis have been reported in post-marketing surveillance.
Do not take Erlonat if you are pregnant. It could harm the unborn baby. Use effective birth control while you are taking this medication and for at least 2 weeks after your treatment ends.
Before taking Erlonat, tell your doctor if you have lung problems (other than lung cancer), kidney or liver disease, if you are dehydrated, or if you smoke.
To be sure this medication is helping your condition and not causing harmful effects, your blood will need to be tested often. This will help your doctor determine how long to treat you with Erlonat. Visit your doctor regularly.
Avoid exposure to sunlight or tanning beds. Erlonat can cause skin rash, dryness, or other irritation. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors. Avoid using skin products that can cause dryness or irritation.
Stop taking Erlonat and call your doctor at once if you have new or worsening lung problems (chest pain, dry cough with fever, wheezing, feeling short of breath), chest pain spreading to the arm or shoulder, sudden numbness or weakness, eye pain or irritation, rapid weight gain, urinating less than usual or not at all, severe or ongoing diarrhea or vomiting, coughing up blood, black or bloody stools, pale skin, easy bruising or bleeding, mouth sores, or a severe skin rash.
There are many other drugs that can interact with Erlonat. Tell your doctor about all medications you use. Keep a list of all your medicines and show it to any healthcare provider who treats you.
The results of a survey conducted on ndrugs.com for Erlonat are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Erlonat. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
Consumer reported useful
No survey data has been collected yet
1 consumer reported price estimates
Was the price you paid to purchase the drug reasonable? Did you feel it was expensive? The below mentioned numbers have been reported by ndrugs.com website users about whether the Erlonat drug is expensive or inexpensive. There is a mixed opinion among users. The rating about the cost of the drug depends on factors like which brand drug the patient purchased, how effective it was for the price paid, the country or place the drug is marketed, and the economic condition of the patient. The users who feel the drug is expensive can look for an alternative brand drug or a generic drug to save the cost.
1 consumer reported time for results
To what extent do I have to use Erlonat before I begin to see changes in my health conditions? As part of the reports released by ndrugs.com website users, it takes 2 days and a few days before you notice an improvement in your health conditions. Please note, it doesn't mean you will start to notice such health improvement in the same time frame as other users. There are many factors to consider, and we implore you to visit your doctor to know how long before you can see improvements in your health while taking Erlonat. To get the time effectiveness of using Erlonat drug by other patients, please click here.
1 consumer reported age
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Information checked by Dr. Sachin Kumar, MD Pharmacology