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Brand Name :
Juxtapid, Lojuxta
Synonyms :
lomitapidum
Class :
Antihyperlipidemic agents
Brand Name :
Juxtapid, Lojuxta
Synonyms :
lomitapidum
Class :
Antihyperlipidemic agents
Dosing forms and strengths
Capsule
5 mg
10 mg
20 mg
30 mg
Starting dose: 5 mg taken orally once daily
Maintenance dose: 5 to 60 mg taken orally once daily, which should be tailored to the individual patient's treatment goals and response to therapy
Maximum dose: 60 mg taken orally once daily
Homozygous Familial Hypercholesterolemia
Starting dose: 5 mg taken orally once daily
Maintenance dose: 5 to 60 mg taken orally once daily, which should be tailored to the individual patient's treatment goals and response to therapy
Maximum dose: 60 mg taken orally once daily
Safety and efficacy are not established
Refer to the adult dosing
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
may enhance the concentration of serum when combined with lomitapide.
It may diminish the absorption when combined with bile acid sequestrants
lomitamide: they may enhance the serum concentration of CYP2D6 Inhibitors
lomitamide: they may enhance the serum concentration of CYP2D6 Inhibitors
lomitamide: they may enhance the serum concentration of CYP2D6 Inhibitors
lomitamide: they may enhance the serum concentration of CYP2D6 Inhibitors
lomitamide: they may enhance the serum concentration of CYP2D6 Inhibitors
when both drugs are combined, there may be an increased effect of lomitapide by affecting hepatic or intestinal enzyme cyp3a4 metabolism
lomitapide increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increased effect of Lomitapide by affecting hepatic or intestinal enzyme CYP3A4 metabolism
when both drugs are combined, there may be an increase in levels of lomitapide by affecting hepatic or intestinal enzyme cyp3a4 metabolism
may enhance the serum concentration when combined
may enhance the serum concentration of CYP3A4 Inhibitors
may increase the CNS depressant effect of CNS Depressants
may enhance the concentration of serum when combined with lomitapide
cyproterone and ethinyl estradiol
may diminish the serum concentration when combined
by affecting intestinal metabolism, the effect of lomitapide may be increased
lomitapide: they may enhance the serum concentration of CYP3A Inhibitors
lomitapide: they may enhance the serum concentration of CYP3A Inhibitors
lomitapide: they may enhance the serum concentration of CYP3A Inhibitors
lomitapide: they may enhance the serum concentration of CYP3A Inhibitors
lomitapide: they may enhance the serum concentration of CYP3A Inhibitors
when both drugs are combined, there may be an increased risk or severity of adverse effects
it may diminish the metabolism when combined with zuclopenthixol
lomitapide: they may increase the CNS depressant effect of CNS Depressants
lomitapide: they may increase the CNS depressant effect of CNS Depressants
lomitapide: they may increase the CNS depressant effect of CNS Depressants
lomitapide: they may increase the CNS depressant effect of CNS Depressants
lomitapide: they may increase the CNS depressant effect of CNS Depressants
When abametapir is used together with lomitapide, this leads to enhanced concentration serum of lomitapide.
When acetazolamide is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When adagrasib is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When aldesleukin is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When asciminib is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When avacopan is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When cannabidiol is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When capsaicin is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When chloramphenicol is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When clofazimine is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When darunavir is used together with lomitapide, this leads to enhanced concentration serum of lomitapide
When abatacept is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When aminoglutethimide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When amobarbital is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When anakinra is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When apremilast is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When armodafinil is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When asunaprevir is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When beclomethasone dipropionate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When bexarotene is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When bosentan is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When budesonide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When butalbital is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When calcitriol is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When canakinumab is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When carbamazepine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When cefradine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When cerivastatin is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When chlorpromazine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When clobazam is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When clobetasol propionate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When clofibrate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When corticotropin is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When cortisone acetate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When cyclophosphamide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When deferasirox is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When deflazacort is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When dexamethasone acetate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When dicloxacillin is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When difluocortolone is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When echinacea is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When enasidenib is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When encorafenib is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When esketamine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When eslicarbazepine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When eslicarbazepine acetate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When estradiol acetate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When estradiol benzoate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When estradiol dienanthate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When estradiol valerate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When etanercept is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When etravirine is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When felbamate is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When flucloxacillin is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When flunisolide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When fluocinolone acetonide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When fluocinonide is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When fluocortolone is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When formestane is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
When fosphenytoin is used together with lomitapide, this leads to an enhancement in lomitapide’s metabolism
when both drugs are combined, there may be a reduced excretion rate of topotecan and result in an elevated level of serum concentration
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
the effect of lomitapide is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
increases the serum concentration of cabazitaxel by MDR1 efflux transporter
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporter
It may enhance the risk of adverse effects when combined with antihyperlipidemic
It may enhance the risk of adverse effects when combined with antihyperlipidemic
It may enhance the risk of adverse effects when combined with antihyperlipidemic
fluoxetine increases the concentration of lomitapide
Actions and Spectrum
The mechanism of action of lomitapide is based on the inhibition of a microsomal triglyceride transfer protein (MTP) involved in lipoprotein synthesis and secretion in the liver. By exerting its action on MTP, lomitapide lowers the creation of very low-density lipoproteins (VLDL) and low density lipoproteins (LDL) which is the major transporter of cholesterol in circulation. Therefore, the drug is used to decrease the total cholesterol, low density lipoprotein cholesterol, and triglyceride concentrations in the blood.
Currently, the spectrum of lomitapide is only applicable in the management of a rare genetic disorder known as familial hypercholesterolemia that affects approximately one in every 200 to 500 people globally.
Frequency defined
>10 %
Adults
Chest pain (24%)
Angina pectoris (10%)
Palpitations (10 %)
Diarrhea (79 %)
Nausea (65%)
Dyspepsia (38%)
Vomitting (34%)
Abdominal distention (21%)
Constipation (21%)
Flatulence (21%)
Rectal tenesmus (10%)
Defecation urgency (10%)
Gastroesophageal reflux disease (10%)
Weight loss (24%)
Black Box Warning
The FDA has included a black box warning for lomitapide where the administration of the drug is linked to severe liver injury, liver failure and deaths. Hepatotoxicity is more likely to occur in cases of concomitant liver disease or excessive alcohol intake.
Contraindication/Caution
Hepatic impairment
Renal impairment
Pregnancy/Lactation
Pregnancy warnings:
Pregnancy category: Insufficient data available
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Pharmacology
lomitapide undergoes relatively fast absorption when taken orally and after 4 hours the drug reaches its peak plasma level. This drug is highly protein bound to plasma proteins particularly to albumin and heavily metabolized by the liver’s cytochrome P450 (CYP) system particularly by the CYP3A4/CYP2C8 enzymes. Its principal metabolite M1 has a pharmacological activity and is involved in the stimulation of cholesterol-lowering action.
Pharmacodynamics
The pharmacodynamics method of lomitapide is the reduction of the microsomal triglyceride transfer protein (MTP) in the liver. MTP is involved in the synthesis and secretion of Very-Low-Density-Lipoprotein (VLDL) particles, which are the precursors of Low-Density-Lipoprotein (LDL) particles – the primary carriers of cholesterol in blood circulation.
Pharmacokinetics
Absorption
It is absorbed through passive diffusion across the intestinal epithelium.
Distribution
It is mainly distributed to the liver as the drug is primarily metabolized in the liver by the cytochrome P450 enzymes CYP3A4 and CYP2C8.
Metabolism
The major metabolite of lomitapide is M1, which is pharmacologically active and contributes to the drug’s lipid-lowering effects.
Elimination and Excretion
It is primarily excreted in the feces, with only a small amount excreted in the urine.
Half-life is approximately 45 hours
Administration
It is taken orally in the form of tablets
Patient information leaflet
Generic Name: lomitapide
Why do we use lomitapide?
It is indicated for homozygous familial hypercholesterolemia patients who are at least 12 years old and should be taken in combination with a low-fat diet and other medications to lower cholesterol. It reduces low-density lipoprotein (LDL) and non-high-density lipoprotein (non-HDL) cholesterol, which are ‘bad’ forms of cholesterol, and the protein that carries the cholesterol in the blood.
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