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Xermelo
Overview
What is Xermelo?
Xermelo (telotristat ethyl) tablets contain telotristat ethyl as telotristat etiprate, a tryptophan hydroxylase inhibitor. Telotristat etiprate is the hippurate salt of telotristat ethyl [(S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate], which undergoes hydrolysis to the active metabolite, (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid.
The molecular formula of telotristat etiprate is CHClFNO CHNO and its molecular weight is 754.2. The molecular weight of the free base (telotristat ethyl) is 575.0.
Chemical Structure:
Telotristat etiprate is a white to off-white solid. The solubility is a function of pH at 25°C; at pH 1 (0.1N HCl), the solubility is greater than 71 mg/mL., at pH 3 phosphate buffer, the solubility is 0.30 mg/mL, at a pH of 5 to 9, the solubility is negligible. In organic solvents, telotristat etiprate is freely soluble in methanol, soluble in acetone, and sparingly soluble in ethanol.
Each Xermelo tablet contains 250 mg of telotristat ethyl (free base) which is equivalent to 328 mg telotristat etiprate. The inactive ingredients of Xermelo tablets include: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, macrogol/PEG, magnesium stearate, polyvinyl alcohol [part hydrolyzed], talc and titanium dioxide.
What does Xermelo look like?
What are the available doses of Xermelo?
Tablets: 250 mg telotristat ethyl ()
What should I talk to my health care provider before I take Xermelo?
How should I use Xermelo?
Xermelo is indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.
The recommended dosage of Xermelo in adult patients is 250 mg three times daily for patients whose diarrhea is inadequately controlled by SSA therapy.
Administration
What interacts with Xermelo?
Sorry No Records found
What are the warnings of Xermelo?
Sorry No Records found
What are the precautions of Xermelo?
Sorry No Records found
What are the side effects of Xermelo?
Sorry No records found
What should I look out for while using Xermelo?
None.
What might happen if I take too much Xermelo?
Sorry No Records found
How should I store and handle Xermelo?
StorageStore at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. StorageStore at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.Xodol is supplied as follows:5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-912-10.7.5 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "7.5" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-913-10.10 mg/300 mgWhite, capsule-shaped, bisected tablets, debossed "10" score "300" on one side and "TP" on the other side in bottles of 100 tablets, NDC 59630-911-10.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].Dispense in a tight, light-resistant container as defined in the USP with a child-resistant closure.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate limiting step in serotonin biosynthesis. The inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea.
Non-Clinical Toxicology
None.Inhibitors of CYP3A4 and CYP2D6
The concomitant use of hydrocodone bitartrate and acetaminophen tablets and CYP3A4 inhibitors, such as macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g. ketoconazole), and protease inhibitors (e.g., ritonavir), can increase the plasma concentration of the hydrocodone from hydrocodone bitartrate and acetaminophen tablets, resulting in increased or prolonged opioid effects. These effects could be more pronounced with concomitant use of hydrocodone bitartrate and acetaminophen tablets and both CYP3A4 and CYP2D6 inhibitors, particularly when an inhibitor is added after a stable dose of hydrocodone bitartrate and acetaminophen tablets is achieved [see ].
After stopping a CYP3A4 inhibitor, as the effects of the inhibitor decline, the hydrocodone plasma concentration will decrease [see ], resulting in decreased opioid efficacy or a withdrawal syndrome in patients who had developed physical dependence to hydrocodone bitartrate and acetaminophen tablets.
If concomitant use is necessary, consider dosage reduction of hydrocodone bitartrate and acetaminophen tablets until stable drug effects are achieved. Follow patients for respiratory depression and sedation at frequent intervals. If a CYP3A4 inhibitor is discontinued, consider increasing the hydrocodone bitartrate and acetaminophen tablets dosage until stable drug effects are achieved. Follow for signs or symptoms of opioid withdrawal.
Inducers of CYP3A4
The concomitant use of hydrocodone bitartrate and acetaminophen tablets and CYP3A4 inducers, such as rifampin, carbamazepine, and phenytoin, can decrease the plasma concentration of hydrocodone [see ], resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to hydrocodone [see ].
After stopping a CYP3A4 inducer, as the effects of the inducer decline, the hydrocodone plasma concentration will increase [see ], which could increase or prolong both the therapeutic effects and adverse reactions, and may cause serious respiratory depression.
If concomitant use is necessary, consider increasing the hydrocodone bitartrate and acetaminophen tablets dosage until stable drug effects are achieved. Follow the patient for signs and symptoms of opioid withdrawal. If a CYP3A4 inducer is discontinued, consider hydrocodone bitartrate and acetaminophen tablets dosage reduction and follow for signs of respiratory depression.
Benzodiazepines and Other CNS Depressants
Due to additive pharmacologic effect, the concomitant use of benzodiazepines and other CNS depressants, such as benzodiazepines and other sedative hypnotics, anxiolytics, and tranquilizers, muscle relaxants, general anesthetics, antipsychotics, and other opioids, including alcohol, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death.
Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients closely for signs of respiratory depression and sedation [see ].
Serotonergic Drugs
The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system, such as selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, 5-HT3 receptor antagonists, drugs that affect the serotonin neurotransmitter system (e.g., mirtazapine, trazodone, tramadol), and monoamine oxidase (MAO) inhibitors (those intended to treat psychiatric disorders and also others, such as linezolid and intravenous methylene blue), has resulted in serotonin syndrome [see ].
If concomitant use is warranted, carefully follow the patient, particularly during treatment initiation and dose adjustment. Discontinue hydrocodone bitartrate and acetaminophen tablets if serotonin syndrome is suspected.
Monoamine Oxidase Inhibitors (MAOIs)
The concomitant use of opioids and MAOIs, such as phenelzine, tranylcypromine, or linezolid, may manifest as serotonin syndrome, or opioid toxicity (e.g., respiratory depression, coma) [see ].
The use of hydrocodone bitartrate and acetaminophen tablets is not recommended for patients taking MAOIs or within 14 days of stopping such treatment.
If urgent use of an opioid is necessary, use test doses and frequent titration of small doses to treat pain while closely monitoring blood pressure and signs and symptoms of CNS and respiratory depression.
Mixed Agonist/Antagonist and Partial Agonist Opioid Analgesics
The concomitant use of opioids with other opioid analgesics, such as butorphanol, nalbuphine, pentazocine, may reduce the analgesic effect of hydrocodone bitartrate and acetaminophen tablets and/or precipitate withdrawal symptoms.
Advise patient to avoid concomitant use of these drugs.
Muscle Relaxants
Hydrocodone bitartrate and acetaminophen tablets may enhance the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression.
If concomitant use is warranted, monitor patients for signs of respiratory depression that may be greater than otherwise expected and decrease the dosage of hydrocodone bitartrate and acetaminophen tablets and/or the muscle relaxant as necessary.
Diuretics
Opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone.
If concomitant use is warranted, follow patients for signs of diminished diuresis and/or effects on blood pressure and increase the dosage of the diuretic as needed.
Anticholinergic Drugs
The concomitant use of anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus.
If concomitant use is warranted, follow patients for signs and symptoms of urinary retention or reduced gastric motility when hydrocodone bitartrate and acetaminophen tablets are used concomitantly with anticholinergic drugs.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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