U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C39H37F6N3O2
Molecular Weight 693.7204
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LOMITAPIDE

SMILES

FC(F)(F)CNC(=O)C4(CCCCN1CCC(CC1)NC(=O)C2=C(C=CC=C2)C3=CC=C(C=C3)C(F)(F)F)C5=CC=CC=C5C6=C4C=CC=C6

InChI

InChIKey=MBBCVAKAJPKAKM-UHFFFAOYSA-N
InChI=1S/C39H37F6N3O2/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49)

HIDE SMILES / InChI
Molecular Formula C39H37F6N3O2
Molecular Weight 693.7204
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://www.everipedia.com/Lomitapide/

Lomitapide (INN, marketed as Juxtapid in the US and as Lojuxta in the EU) is a drug for the treatment of familial hypercholesterolemia, developed by Aegerion Pharmaceuticals. It has been tested in clinical trials as single treatment and in combinations with atorvastatin, ezetimibe and fenofibrate. The US Food and Drug Administration (FDA) approved lomitapide on 21 December 2012, as an orphan drug to reduce LDL cholesterol, total cholesterol, apolipoprotein B, and non-high-density lipoprotein (non-HDL) cholesterol in patients with homozygous familial hypercholesterolemia (HoFH). On 31 May 2013 the European Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion with a unanimous vote recommending a marketing authorization for lomitapide. On 31 July 2013 the European Commission approved lomitapide as an adjunct to a low-fat diet and other lipid-lowering medicinal products with or without low density lipoprotein (LDL) apheresis in adult patients with HoFH. UXTAPID directly binds and inhibits microsomal triglyceride transfer protein (MTP), which resides in the lumen of the endoplasmic reticulum, thereby preventing the assembly of apo B containing lipoproteins in enterocytes and hepatocytes. This inhibits the synthesis of chylomicrons and VLDL. The inhibition of the synthesis of VLDL leads to reduced levels of plasma LDL-C.

Originator

Approval Year

2012
608
Targets

Targets

Primary TargetPharmacologyConditionPotency
Microsomal triglyceride transfer protein large subunit
4
Target ID: P55157
Gene ID: 4547.0
Gene Symbol: MTTP
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 8.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8583
JUXTAPID

Approved Use

Indicated as an adjunct to a low-fat diet and other lipid-lowering treatments, including LDL apheresis where available, to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with homozygous familial hypercholesterolemia (HoFH). Limitations of use: the safety and effectiveness of JUXTAPID have not been established in patients with hypercholesterolemia who do not have HoFH. The effect of JUXTAPID on cardiovascular morbidity and mortality has not been determined.

Launch Date

2012
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.13 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
0.986 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
1.03 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
2.74 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
2.52 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
2.65 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
28.6 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
30.2 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
31 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
5.75 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
24.6 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
43.6 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
38.3 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
40.2 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
75.2 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
70.4 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
72.9 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
460 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
443 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
450 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
241 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
403 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
48.8 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
52.4 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
47.7 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: healthy
age:
sex:
food status:
39.1 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
38.7 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
37 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M1 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
44 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
46 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
45.7 h
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT02044419
20 mg single, oral
dose: 20 mg
route of administration: oral
experiment type: single
co-administered:
LOMITAPIDE METABOLITE M3 plasma
Homo sapiens
population: healthy
age:
sex:
food status:
51.5 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
46.5 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26686567/
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.2%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203858s019lbl.pdf
60 mg 1 times / day unknown, oral
dose: 60 mg
route of administration: Oral
experiment type: UNKNOWN
co-administered:
LOMITAPIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Disc. AE: Diarrhea, Abdominal pain...
Other AEs: Alanine aminotransferase increase, Aspartate aminotransferase increase...
AEs leading to
discontinuation/dose reduction:
Diarrhea (7%)
Abdominal pain (3%)
Nausea (3%)
Gastroenteritis (3%)
Weight loss (3%)
Headache (3%)
Uncontrolled INR (3%)
Other AEs:
Alanine aminotransferase increase (34%)
Aspartate aminotransferase increase (34%)
Fatty liver (6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Disc. AE: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (5 patients)
Nausea (3 patients)
Abdominal discomfort (3 patients)
Vomiting (1 patient)
Diarrhea (5 patients)
Vomiting (4 patients)
Nausea (3 patients)
Gastroenteritis (3 patients)
Influenza (2 patients)
Chest pain (2 patients)
Pyrexia (2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
200 mg single, oral
Highest studied dose
Dose: 200 mg
Route: oral
Route: single
Dose: 200 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
healthy
Health Status: healthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
healthy
Health Status: healthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Abdominal pain 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Gastroenteritis 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Headache 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Nausea 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Uncontrolled INR 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Weight loss 3%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Alanine aminotransferase increase 34%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Aspartate aminotransferase increase 34%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Fatty liver 6%
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Diarrhea 7%
Disc. AE
5 mg 1 times / day steady, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203858s000lbl.pdf
Vomiting 1 patient
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Chest pain 2 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Influenza 2 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Pyrexia 2 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Abdominal discomfort 3 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Gastroenteritis 3 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Nausea 3 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Nausea 3 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Vomiting 4 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Diarrhea 5 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Diarrhea 5 patients
Disc. AE
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
unhealthy, 30.7 years (range: 18 - 55 years)
Health Status: unhealthy
Age Group: 30.7 years (range: 18 - 55 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Headache 1 patient
Disc. AE
100 mg single, oral
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
healthy
Health Status: healthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203858Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
1087

inhibitor
2252

substrate
1946
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741

CYP1A2
2153

CYP2B6
926

CYP2C19
2057

CYP2E1
1060

BCRP
910

OATP1B1
1079

OATP1B3
961

OCT1
620

OAT1
725

OAT3
747

OCT2
779
CYP1A2
1197

CYP2B6
776

CYP2C8
810

CYP2C19
1119

P-gp
2052

CYP2E1
729
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no
CYP1A2
2333
 no
CYP1A2
2333
 no
CYP2B6
1160
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C9
2497
 no
CYP2D6
2546
 no
CYP2E1
1146
 no
CYP3A4
2633
 no
OAT1
730
 no
OAT3
749
 no
OATP1B1
1095
 no
OATP1B3
970
 no
OCT1
656
 no
OCT2
782
 no
P-gp
1932
 yes [IC50 0.62 uM]
CYP3A4
2633
 yes [IC50 8 uM]
weak (co-administration study)
Comment: lomitapide increased simvastatin cmax/auc ~2x
Page: 22.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1946
 major
yes (co-administration study)
Comment: ketoconazole increased lomitapide exposure 27x
Page: 23.0
P-gp
2052
 no
CYP1A2
1197
 weak
CYP2B6
776
 weak
CYP2C19
1119
 weak
CYP2C8
810
 weak
CYP2E1
729
 weak
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:72297
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:72297
ChemicalBook
CB62485047
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62485047
MolPort
MolPort-028-754-209
https://www.molport.com/shop/molecule-link/MolPort-028-754-209
ZINC
ZINC000027990463
http://zinc15.docking.org/substances/ZINC000027990463
PubMed

PubMed

TitleDatePubMed
Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolaemia: a single-arm, open-label, phase 3 study.
2013-01-05
Lomitapide, a microsomal triglyceride transfer protein inhibitor for the treatment of hypercholesterolemia.
2010-02
Gateways to clinical trials.
2009-06
Inhibition of microsomal triglyceride transfer protein in familial hypercholesterolemia.
2007-01-11
A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.
2001-03-15
Patents

Patents

CN103690960A
2
EP1725234B9
2
US2007088089
2
US2007093468
2
US2011112097
2
WO2015121877A2
2

Sample Use Guides

In Vivo Use Guide
Initiate treatment at 5 mg once daily. Titrate dose based on acceptable safety/tolerability: increase to 10 mg daily after at least 2 weeks; and then, at a minimum of 4-week intervals, to 20 mg, 40 mg, and up to the maximum recommended dose of 60 mg daily. Take once daily, whole, with water and without food, at least 2 hours after evening meal.
Route of Administration: Oral
In Vitro Use Guide
In in vitro experiments using unilamellar vesicles, lomitapide inhibited rat, hamster, and human MTP with an inhibitory concentration of 50% (IC50) of 5 to 7 nmol/L. In vitro studies demonstrated a reduction in apoB secretion by hepatocytes on treatment with lomitapide
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:42:42 GMT 2025
Edited
by admin
on Mon Mar 31 18:42:42 GMT 2025
Record UNII
82KUB0583F
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
JUXTAPID
Preferred Name English
LOMITAPIDE
DASH   INN   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
AEGR-733
Code English
LOMITAPIDE [MI]
Common Name English
9H-FLUORENE-9-CARBOXAMIDE, N-(2,2,2-TRIFLUOROETHYL)-9-(4-(4-(((4'-(TRIFLUOROMETHYL)(1,1'-BIPHENYL)-2-YL)CARBONYL)AMINO)-1-PIPERIDINYL)BUTYL)-
Systematic Name English
LOMITAPIDE [USAN]
Common Name English
N-(2,2,2-TRIFLUOROETHYL)-9-(4-(4-(((4'-(TRIFLUOROMETHYL)BIPHENYL-2-YL)CARBONYL)AMINO)PIPERIDIN-1-YL)BUTYL)-9H-FLUORENE-9-CARBOXAMIDE
Systematic Name English
lomitapide [INN]
Common Name English
BMS-201038-01
Code English
Lomitapide [WHO-DD]
Common Name English
LOMITAPIDE [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29703
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
NDF-RT N0000186779
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
FDA ORPHAN DRUG 245907
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
EU-Orphan Drug EU/3/10/823
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
WHO-VATC QC10AX12
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
WHO-ATC C10AX12
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
FDA ORPHAN DRUG 332110
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
Code System Code Type Description
WIKIPEDIA
LOMITAPIDE
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
USAN
TT-134
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
NDF-RT
N0000185503
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY P-Glycoprotein Inhibitors [MoA]
SMS_ID
100000128162
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
INN
9120
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
DAILYMED
82KUB0583F
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
EVMPD
SUB34920
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
RXCUI
1364479
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY RxNorm
IUPHAR
7439
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
CHEBI
72297
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
CHEBI
72299
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
MERCK INDEX
m11671
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
DRUG CENTRAL
4721
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
HSDB
8218
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
NDF-RT
N0000182141
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
PUBCHEM
9853053
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
ChEMBL
CHEMBL354541
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
DRUG BANK
DB08827
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
NDF-RT
N0000186778
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY Microsomal Triglyceride Transfer Protein Inhibitors [MoA]
EPA CompTox
DTXSID50171294
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
NCI_THESAURUS
C83891
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
FDA UNII
82KUB0583F
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
LACTMED
Lomitapide
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
CAS
182431-12-5
Created by admin on Mon Mar 31 18:42:42 GMT 2025 , Edited by admin on Mon Mar 31 18:42:42 GMT 2025
PRIMARY
Related Record Type Details
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> NON-INHIBITOR
MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN LARGE SUBUNIT
TARGET -> INHIBITOR
In the small unilamellar vesicle (SUV) assay, IC50 values for isolated human MTP 5 nM.
IC50
CYTOCHROME P450 2C19
METABOLIC ENZYME -> SUBSTRATE
MINOR
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
MINOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
Lomitapide is a weak in vivo CYP3A inhibitor.
WEAK
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> NON-SUBSTRATE
Structure of LOMITAPIDE
EXCRETED UNCHANGED
FECAL
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
CYTOCHROME P450 2B6
METABOLIC ENZYME -> SUBSTRATE
MINOR
CYTOCHROME P450 1A2
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
Structure of N-(PIPERIDIN-4-YL)-4'-(TRIFLUOROMETHYL)-BIPHENYL-2-CARBOXAMIDE
METABOLITE -> PARENT
In plasma, M1 was the prominent metabolite that accounted for 5.75% of the total radioactivity in 0 – 24 hours plasma samples. In urine, M1 was the prominent metabolite that accounted for 4.69% of the dose in the 0 –96 hours urine samples. In feces, M1 was the minor metabolite that accounted for 0.49%of the dose in the 0 – 96 hours feces.
FECAL; PLASMA; URINE
Structure of 3,4,5-TRIHYDROXY-6-(4-(9-(2,2,2-TRIFLUOROETHYLCARBAMOYL)FLUOREN-9-YL)BUTANOYLOXY)TETRAHYDROPYRAN-2-CARBOXYLIC ACID, (2S,3S,4S,5R,6S)-
METABOLITE -> PARENT
In plasma, M10+M18 accounted for 9.67% (combined) of the total radioactivity in 0 – 24 hours plasma samples. In urine, M18 was the prominent metabolite, which accounted for 3.77% of the dose in the 0 – 96 hours urine samples.
PLASMA; URINE
Structure of 9-(4-(4-AMINO-1-PIPERIDINYL)BUTYL)-N-(2,2,2-TRIFLUOROETHYL)-9H-FLUORENE-9-CARBOXAMIDE
METABOLITE -> PARENT
MINOR
Structure of N-(2-OXO-4-PIPERIDYL)-2-(4-(TRIFLUOROMETHYL)PHENYL)BENZAMIDE
METABOLITE -> PARENT
MINOR
FECAL; URINE
Structure of N-(2,2,2-TRIFLUORO-1-HYDROXY-ETHYL)-9-(4-(4-((2-(4-(TRIFLUOROMETHYL)PHENYL)BENZOYL)AMINO)-1-PIPERIDYL)BUTYL)FLUORENE-9-CARBOXAMIDE
METABOLITE -> PARENT
Structure of 9-(4-(4-((2-(4-(TRIFLUOROMETHYL)PHENYL)BENZOYL)AMINO)-1-PIPERIDYL)BUTYL)FLUORENE-9-CARBOXAMIDE
METABOLITE -> PARENT
Structure of 9-(4-(1-OXIDO-4-(((4'-(TRIFLUOROMETHYL)(1,1'-BIPHENYL)-2-YL)CARBONYL)AMINO)-1-PIPERIDINYL)BUTYL)-N-(2,2,2-TRIFLUOROETHYL)-9H-FLUORENE-9-CARBOXAMIDE
METABOLITE -> PARENT
Structure of 2-(4-(TRIFLUOROMETHYL)PHENYL)BENZAMIDE
METABOLITE -> PARENT
MINOR
PLASMA
Structure of 3,4,5-TRIHYDROXY-6-(4-(9-(2,2,2-TRIFLUOROETHYLCARBAMOYL)FLUOREN-9-YL)BUTOXY)TETRAHYDROPYRAN-2-CARBOXYLIC ACID, (2S,3S,4S,5R,6R)-
METABOLITE -> PARENT
In plasma, M10+M18 accounted for 9.67% (combined) of the total radioactivity in 0 – 24 hours plasma samples. In urine, M10 was the minor metabolite, which accounted for 0.33% of the dose in the 0 – 96 hours urine samples.
PLASMA; URINE
Structure of 9-(4-AMINOBUTYL)-N-(2,2,2-TRIFLUOROETHYL)-9H-FLUORENE-9-CARBOXAMIDE
METABOLITE -> PARENT
In plasma, M5 was the prominent metabolite that accounted for 4.26% of the total radioactivity in 0 – 24 hours plasma samples. In urine, M5 was the prominent metabolite that accounted for 3.47% of the dose in the 0 –96 hours urine samples. In feces, M5 was the minor metabolite that accounted for 0.78% of the dose in the 0 – 96 hours feces.
FECAL; PLASMA; URINE
Structure of 4-(9-(2,2,2-TRIFLUOROETHYLCARBAMOYL)FLUOREN-9-YL)BUTANOIC ACID
METABOLITE -> PARENT
In plasma, M3 was the major metabolite that accounted for 17.3% of the plasma radioactivity. In urine, M3 was the minor metabolite that accounted for 0.34% of the dose in the 0 –96 hours urine samples. In feces, M3 was the minor metabolite that accounted for 1.33 % of the dose in the 0 – 96 hours feces.
FECAL; PLASMA; URINE
Related Record Type Details
Structure of LOMITAPIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC SINGLE DOSE

ORAL ADMINISTRATION

Tmax PHARMACOKINETIC ORAL ADMINISTRATION

SINGLE DOSE

Volume of Distribution PHARMACOKINETIC SINGLE DOSE

ORAL ADMINISTRATION

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