lomitapide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
microsomal triglyceride transfer protein (MTP) inhibitors	4721	182431-12-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lomitapide juxtapid BMS-201038 lomitapide mesylate lojuxta lomitapide mesilate BMS201038 BMS 201038	an anticholesteremic agent and microsomal triglycide transfer protein inhibitor Molecular weight: 693.73 Formula: C39H37F6N3O2 CLOGP: 6.69 LIPINSKI: 2 HAC: 5 HDO: 2 TPSA: 61.44 ALOGS: -6.89 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lomitapide
juxtapid
BMS-201038
lomitapide mesylate
lojuxta
lomitapide mesilate
BMS201038
BMS 201038

an anticholesteremic agent and microsomal triglycide transfer protein inhibitor

Molecular weight: 693.73
Formula: C39H37F6N3O2
CLOGP: 6.69
LIPINSKI: 2
HAC: 5
HDO: 2
TPSA: 61.44
ALOGS: -6.89
ROTB: 12

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	39.70 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	16.30 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0.07 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 21, 2012	FDA	AEGERION

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy cessation	1121.66	38.88	278	3657	30179	63454908
Weight decreased	424.92	38.88	243	3692	276555	63208532
Diarrhoea	383.33	38.88	328	3607	715038	62770049
Flatulence	208.59	38.88	79	3856	34623	63450464
Low density lipoprotein increased	202.63	38.88	52	3883	6305	63478782
Diet noncompliance	148.45	38.88	25	3910	368	63484719
Nausea	120.17	38.88	199	3736	854272	62630815
Abdominal pain upper	109.12	38.88	95	3840	206349	63278738
Inappropriate schedule of product administration	99.16	38.88	68	3867	103897	63381190
Product dose omission issue	83.95	38.88	87	3848	234226	63250861

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy cessation	494.43	54.04	125	1764	16848	34938194
Weight decreased	345.41	54.04	173	1716	176128	34778914
Diarrhoea	205.64	54.04	167	1722	389745	34565297
Flatulence	125.55	54.04	46	1843	21152	34933890
Diet noncompliance	122.51	54.04	19	1870	187	34954855
Low density lipoprotein increased	110.53	54.04	29	1860	4407	34950635
Product dose omission issue	94.72	54.04	66	1823	119645	34835397
Abdominal discomfort	64.21	54.04	40	1849	59795	34895247
Blood cholesterol increased	60.46	54.04	27	1862	20516	34934526

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy cessation	1263.86	41.38	316	4395	37246	79702431
Weight decreased	538.38	41.38	304	4407	354894	79384783
Diarrhoea	449.86	41.38	385	4326	880104	78859573
Flatulence	264.09	41.38	98	4613	42626	79697051
Low density lipoprotein increased	222.25	41.38	59	4652	8563	79731114
Nausea	151.07	41.38	229	4482	956967	78782710
Abdominal pain upper	126.69	41.38	105	4606	223714	79515963
Diet noncompliance	113.97	41.38	21	4690	556	79739121
Product dose omission issue	101.88	41.38	97	4614	247440	79492237
Inappropriate schedule of product administration	97.72	41.38	73	4638	133555	79606122

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C10AX12	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Other lipid modifying agents
CHEBI has role	CHEBI:35821	anticholesteremic drugs
CHEBI has role	CHEBI:72298	microsomal triglyceride transfer protein inhibitor
FDA EPC	N0000186779	Microsomal Triglyceride Transfer Protein Inhibitor
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000186778	Microsomal Triglyceride Transfer Protein Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Familial hypercholesterolemia - homozygous	indication	238078005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.28	acidic
pKa2	13.97	acidic
pKa3	8.71	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	10016404	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	10555938	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	8618135	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	9265758	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	9364470	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	9433617	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	9861622	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 10MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	7932268	Aug. 19, 2027	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 20MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	10016404	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
EQ 20MG BASE	JUXTAPID	AMRYT	N203858	Dec. 21, 2012	RX	CAPSULE	ORAL	10555938	March 7, 2025	A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Microsomal triglyceride transfer protein large subunit	Cytosolic other	P55157	MTP_HUMAN	INHIBITOR	IC50	8.10		WOMBAT-PK	CHEMBL

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External reference:

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ID	Source
014810	NDDF
014811	NDDF
1364478	RXNORM
196706	MMSL
202914-84-9	SECONDARY_CAS_RN
29025	MMSL
30485	MMSL
4032035	VUID
4032035	VANDF
716228008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-105	CAPSULE	5 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-105	CAPSULE	5 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-110	CAPSULE	10 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-110	CAPSULE	10 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-120	CAPSULE	20 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-120	CAPSULE	20 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-130	CAPSULE	30 mg	ORAL	NDA	33 sections
Juxtapid	HUMAN PRESCRIPTION DRUG LABEL	1	76431-130	CAPSULE	30 mg	ORAL	NDA	33 sections

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