Dexilant

• Takeda Pharmaceuticals America, Inc.

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of Dexilant there are no specific foods that you must exclude from your diet when receiving Dexilant.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category B. There are no well-done studies that have been done in humans with Dexilant. In animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

• Store at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• This medicine comes with an extra patient fact sheet called a Medication Guide. Read it with care. Read it again each time Dexilant is refilled. If you have any questions about this medicine, please talk with the doctor, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Dexilant or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Dexilant. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Recommended Dosage in Patients 12 Years of Age and Older

Dosage Adjustment in Patients with Hepatic Impairment for the Healing of Erosive Esophagitis

For patients with moderate hepatic impairment (Child-Pugh Class B), the recommended dosage is a 30 mg Dexilant capsule once daily for up to eight weeks. The use of a Dexilant capsule is not recommended in patients with severe hepatic impairment (Child-Pugh Class C) [see Use in Specific Populations (8.6)].

Important Administration Information

• Missed doses: If a dose is missed, administer as soon as possible. However, if the next scheduled dose is due, do not take the missed dose, and take the next dose on time. Do not take two doses at one time to make up for a missed dose.

Dexilant capsules

• Take without regard to food.
• Swallow whole; do not chew.
• For patients who have trouble swallowing capsules, Dexilant capsules can be opened and administered with applesauce as follows:
  1. Place one tablespoonful of applesauce into a clean container.
  2. Open capsule.
  3. Sprinkle intact granules on applesauce.
  4. Swallow applesauce and granules immediately. Do not chew granules. Do not save the applesauce and granules for later use.
• Alternatively, the capsule can be administered with water via oral syringe or nasogastric (NG) tube.

  Administration with Water in an Oral Syringe

  1. Open the capsule and empty the granules into a clean container with 20 mL of water.
  2. Withdraw the entire mixture into a syringe.
  3. Gently swirl the syringe in order to keep granules from settling.
  4. Administer the mixture immediately into the mouth. Do not save the water and granule mixture for later use.
  5. Refill the syringe with 10 mL of water, swirl gently, and administer.
  6. Refill the syringe again with 10 mL of water, swirl gently, and administer.

  Administration with Water via a NG Tube (≥16 French)

  1. Open the capsule and empty the granules into a clean container with 20 mL of water.
  2. Withdraw the entire mixture into a catheter-tip syringe.
  3. Swirl the catheter-tip syringe gently in order to keep the granules from settling, and immediately inject the mixture through the NG tube into the stomach. Do not save the water and granule mixture for later use.
  4. Refill the catheter-tip syringe with 10 mL of water, swirl gently, and flush the tube.
  5. Refill the catheter-tip syringe again with 10 mL of water, swirl gently, and administer.

• Dexilant is contraindicated in patients with known hypersensitivity to any component of the formulation [see Description (11)]. Hypersensitivity reactions, including anaphylaxis have been reported [see Adverse Reactions (6.1, 6.2)]. Acute interstitial nephritis (AIN) has been reported with other proton pump inhibitors (PPIs), including lansoprazole of which dexlansoprazole is the R-enantiomer.
• PPIs, including Dexilant, are contraindicated with rilpivirine-containing products [see Drug Interactions (7)].

The following serious adverse reactions are described below and elsewhere in labeling:

• Acute Interstitial Nephritis [see Warnings and Precautions (5.2)]
• Clostridium difficile-Associated Diarrhea [see Warnings and Precautions (5.3)]
• Bone Fracture [see Warnings and Precautions (5.4)]
• Cutaneous and Systemic Lupus Erythematosus [see Warnings and Precautions (5.5)]
• Cyanocobalamin (Vitamin B12) Deficiency [see Warnings and Precautions (5.6)]
• Hypomagnesemia [see Warnings and Precautions (5.7)]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Adults

The safety of Dexilant capsules were evaluated in 4548 adult patients in controlled and single-arm clinical trials, including 863 patients treated for at least six months and 203 patients treated for one year. Patients ranged in age from 18 to 90 years (median age 48 years), with 54% female, 85% Caucasian, 8% Black, 4% Asian, and 3% other races. Six randomized controlled clinical trials were conducted for the treatment of EE, maintenance of healed EE, and symptomatic GERD, which included 896 patients on placebo, 455 patients on Dexilant 30 mg capsules, 2218 patients on Dexilant 60 mg capsules, and 1363 patients on lansoprazole 30 mg once daily.

Common Adverse Reactions

The most common adverse reactions (>2%) that occurred at a higher incidence for Dexilant capsules than placebo in the controlled studies are presented in Table 2.

Adverse Reactions Resulting in Discontinuation

In controlled clinical studies, the most common adverse reaction leading to discontinuation from Dexilant capsules was diarrhea (0.7%).

Less Common Adverse Reactions

Other adverse reactions that were reported in controlled studies at an incidence of less than 2% are listed below by body system:

Blood and Lymphatic System Disorders: anemia, lymphadenopathy

Cardiac Disorders: angina, arrhythmia, bradycardia, chest pain, edema, myocardial infarction, palpitation, tachycardia

Ear and Labyrinth Disorders: ear pain, tinnitus, vertigo

Endocrine Disorders: goiter

Eye Disorders: eye irritation, eye swelling

Gastrointestinal Disorders: abdominal discomfort, abdominal tenderness, abnormal feces, anal discomfort, Barrett's esophagus, bezoar, bowel sounds abnormal, breath odor, colitis microscopic, colonic polyp, constipation, dry mouth, duodenitis, dyspepsia, dysphagia, enteritis, eructation, esophagitis, gastric polyp, gastritis, gastroenteritis, gastrointestinal disorders, gastrointestinal hypermotility disorders, GERD, GI ulcers and perforation, hematemesis, hematochezia, hemorrhoids, impaired gastric emptying, irritable bowel syndrome, mucus stools, oral mucosal blistering, painful defecation, proctitis, paresthesia oral, rectal hemorrhage, retching

General Disorders and Administration Site Conditions: adverse drug reaction, asthenia, chest pain, chills, feeling abnormal, inflammation, mucosal inflammation, nodule, pain, pyrexia

Hepatobiliary Disorders: biliary colic, cholelithiasis, hepatomegaly

Immune System Disorders: hypersensitivity

Infections and Infestations: candida infections, influenza, nasopharyngitis, oral herpes, pharyngitis, sinusitis, viral infection, vulvo-vaginal infection

Injury, Poisoning and Procedural Complications: falls, fractures, joint sprains, overdose, procedural pain, sunburn

Laboratory Investigations: ALP increased, ALT increased, AST increased, bilirubin decreased/increased, blood creatinine increased, blood gastrin increased, blood glucose increased, blood potassium increased, liver function test abnormal, platelet count decreased, total protein increased, weight increase

Metabolism and Nutrition Disorders: appetite changes, hypercalcemia, hypokalemia

Musculoskeletal and Connective Tissue Disorders: arthralgia, arthritis, muscle cramps, musculoskeletal pain, myalgia

Nervous System Disorders: altered taste, convulsion, dizziness, headaches, migraine, memory impairment, paresthesia, psychomotor hyperactivity, tremor, trigeminal neuralgia

Psychiatric Disorders: abnormal dreams, anxiety, depression, insomnia, libido changes

Renal and Urinary Disorders: dysuria, micturition urgency

Reproductive System and Breast Disorders: dysmenorrhea, dyspareunia, menorrhagia, menstrual disorder

Respiratory, Thoracic and Mediastinal Disorders: aspiration, asthma, bronchitis, cough, dyspnea, hiccups, hyperventilation, respiratory tract congestion, sore throat

Skin and Subcutaneous Tissue Disorders: acne, dermatitis, erythema, pruritus, rash, skin lesion, urticaria

Vascular Disorders: deep vein thrombosis, hot flush, hypertension

Additional adverse reactions that were reported in a long-term single-arm trial and were considered related to Dexilant by the treating physician included: anaphylaxis, auditory hallucination, B-cell lymphoma, bursitis, central obesity, cholecystitis acute, dehydration, diabetes mellitus, dysphonia, epistaxis, folliculitis, gout, herpes zoster, hyperlipidemia, hypothyroidism, increased neutrophils, MCHC decrease, neutropenia, rectal tenesmus, restless legs syndrome, somnolence, tonsillitis.

Pediatrics

The safety of Dexilant capsules were evaluated in controlled and single-arm clinical trials including 166 pediatric patients,12 to 17 years of age for the treatment of symptomatic non-erosive GERD, healing of EE, maintenance of healed EE and relief of heartburn [see Clinical Studies (14.4)].

The adverse reaction profile was similar to that of adults. The most common adverse reactions that occurred in ≥5% of patients were headache, abdominal pain, diarrhea, nasopharyngitis and oropharyngeal pain.

Other Adverse Reactions

See the full prescribing information for lansoprazole for other adverse reactions not observed with Dexilant.

Postmarketing Experience

The following adverse reactions have been identified during post-approval of Dexilant. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Blood and Lymphatic System Disorders: autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura

Ear and Labyrinth Disorders: deafness

Eye Disorders: blurred vision

Gastrointestinal Disorders: oral edema, pancreatitis

General Disorders and Administration Site Conditions: facial edema

Hepatobiliary Disorders: drug-induced hepatitis

Immune System Disorders: anaphylactic shock (requiring emergency intervention), exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (some fatal)

Infections and Infestations: Clostridium difficile-associated diarrhea

Metabolism and Nutrition Disorders: hypomagnesemia, hyponatremia

Musculoskeletal System Disorders: bone fracture

Nervous System Disorders: cerebrovascular accident, transient ischemic attack

Renal and Urinary Disorders: acute renal failure

Respiratory, Thoracic and Mediastinal Disorders: pharyngeal edema, throat tightness

Skin and Subcutaneous Tissue Disorders: generalized rash, leukocytoclastic vasculitis

The active ingredient in Dexilant (dexlansoprazole) delayed-release capsules, a proton pump inhibitor, is (+)-2-[(R)-{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl] methyl} sulfinyl]-1H-benzimidazole, a compound that inhibits gastric acid secretion. Dexlansoprazole is the R-enantiomer of lansoprazole (a racemic mixture of the R- and S-enantiomers). Its empirical formula is: C16H14F3N3O2S, with a molecular weight of 369.36. Dexlansoprazole has the following chemical structure:

Dexlansoprazole is a white to nearly white crystalline powder which melts with decomposition at 140°C. Dexlansoprazole is freely soluble in dimethylformamide, methanol, dichloromethane, ethanol, and ethyl acetate; and soluble in acetonitrile; slightly soluble in ether; and very slightly soluble in water; and practically insoluble in hexane.

Dexlansoprazole is stable when exposed to light. Dexlansoprazole is more stable in neutral and alkaline conditions than acidic conditions.

Dexlansoprazole is supplied for oral administration as a dual delayed-release formulation in capsules. The capsules contain dexlansoprazole in a mixture of two types of enteric-coated granules with different pH-dependent dissolution profiles [see Clinical Pharmacology (12.3)].

Dexilant delayed-release capsules are available in two dosage strengths: 30 and 60 mg, per capsule. Each capsule contains enteric-coated granules consisting of dexlansoprazole (active ingredient) and the following inactive ingredients: sugar spheres, magnesium carbonate, sucrose, low-substituted hydroxypropyl cellulose, titanium dioxide, hydroxypropyl cellulose, hypromellose 2910, talc, methacrylic acid copolymers, polyethylene glycol 8000, triethyl citrate, polysorbate 80, and colloidal silicon dioxide. The components of the capsule shell include the following inactive ingredients: hypromellose, carrageenan and potassium chloride. Based on the capsule shell color, blue contains FD&C Blue No. 2 aluminum lake; gray contains black ferric oxide; and both contain titanium dioxide.

More frequent side effects include: diarrhea. See below for a comprehensive list of adverse effects.