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Chemical Structure| 182431-12-5 Chemical Structure| 182431-12-5

Structure of Lomitapide
CAS No.: 182431-12-5

Chemical Structure| 182431-12-5

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Lomitapide is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.

Synonyms: AEGR-733; BMS-201038; AEGR 773

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Product Details of Lomitapide

CAS No. :182431-12-5
Formula : C39H37F6N3O2
M.W : 693.72
SMILES Code : O=C(C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C6=C1C=CC=C6)C=CC=C5)NCC(F)(F)F
Synonyms :
AEGR-733; BMS-201038; AEGR 773
MDL No. :MFCD16620494

Safety of Lomitapide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00474240 Hypercholesterolemia Phase 2 Completed - United States, Alabama ... More >> Medical Affiliated Research Center Huntsville, Alabama, United States, 35801 United States, Florida Jacksonville Center for Clinical research Jacksonville, Florida, United States, 32205 Jacksonville Center For Clinical Research Jacksonville, Florida, United States, 32216 Renstar Medical Research Ocala, Florida, United States, 34471 United States, Georgia North Georgia Clinical Research Woodstock, Georgia, United States, 30189 United States, Illinois Radiant Research Chicago, Illinois, United States, 60610 United States, Indiana Medsphere Medical Research Center Evansville, Indiana, United States, 47714 Midwest Institute for Clinical Research Indianapolis, Indiana, United States, 46260 United States, Maine Maine Research Associates Auburn, Maine, United States, 04210 United States, Maryland Health Trends Research Baltimore, Maryland, United States, 21209 United States, North Carolina Piedmont Medical Research Associates Winston-Salem, North Carolina, United States, 27103 United States, Ohio Sterling Research Group Cincinnati, Ohio, United States, 45246 United States, South Carolina Coastal Carolina Research Center Goose Creek, South Carolina, United States, 29445 United States, Texas Dallas Diabetes and Endocrine Center Dallas, Texas, United States, 75230 Diabetes and Glandular Disease Research Dallas, Texas, United States, 78229 United States, Virginia Hampton Roads Center for Clinical Research Norfolk, Virginia, United States, 23502 National Clinical Research Richmond, Virginia, United States, 23294 Less <<
NCT00474240 - Completed - -
NCT00559962 - Completed - -
NCT00359281 Healthy Phase 2 Completed - United States, Pennsylvania ... More >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Less <<
NCT00559962 Hyperlipidemia Phase 2 Completed - United States, California ... More >> Scripps Clinic San Diego, California, United States, 92128 Radiant Research Santa Rosa, California, United States, 95405 United States, District of Columbia MedStar Research Institute Washington, District of Columbia, United States, 20003 United States, Illinois Radiant Research Chicago, Illinois, United States, 60610 United States, Iowa University of Iowa Iowa City, Iowa, United States, 52242 United States, Kentucky LMARC Louisville, Kentucky, United States, 40213 United States, Maine Maine Research Associates Auburn, Maine, United States, 04210 United States, Maryland Health Trends Research Baltimore, Maryland, United States, 21209 Johns Hopkins Baltimore, Maryland, United States, 21287 United States, Missouri Washington Univ. School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Sterling Research Group Cincinnati, Ohio, United States, 45219 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 United States, Texas Baylor College of Medicine Houston, Texas, United States, 77030 Clinical Trial Network Houston, Texas, United States, 77074 dgd Research San Antonio, Texas, United States, 78229 Less <<
NCT00405067 Hypercholesterolemia Phase 2 Completed - United States, New Jersey ... More >> Pharmanet, Inc Princeton, New Jersey, United States, 08540-6242 Less <<
NCT00405067 - Completed - -
NCT00690443 - Completed - -
NCT00690443 Hypercholesterolemia Phase 2 Completed - United States, Florida ... More >> Linda Murray, DO - Radiant Research Pinellas Park, Florida, United States, 33781 United States, Minnesota Sheila Rodstein, MD Edina, Minnesota, United States, 55435 United States, Ohio Dennis McCluskey, MD - Radiant Research Mogadore, Ohio, United States, 44260 United States, Texas Michele Reynolds, MD Dallas, Texas, United States, 75231 William Jennings, MD - Radiant Research San Antonio, Texas, United States, 78229 Less <<
NCT00730236 Homozygous Familial Hyperchole... More >>sterolemia Less << PHASE3 COMPLETED 2025-10-11 Cedars-Sinai Medical Center, L... More >>os Angeles, California, 90048, United States|University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|Robarts Research Institute, London, Ontario, N6A 5K8, Canada|Lipid Clinic and University of Montreal Community Genomic Medicine Center, Chicoutimi, Quebec, G7H 5H6, Canada|Dipartimento di Medicina Clinica e Della Patalogie Emergenti, Palermo, Sicily, Italy|Medicina Interna Universitaria, Ferrara, Italy|Centro Universitario Dislipidemie, Milano, Italy|Dipartimento di Clinica e Terapia Medica, Roma, Italy|Cardiology Research, Bloemfontein, 9300, South Africa|University of Capetown, Cape town, 7925, South Africa Less <<
NCT00730236 Homozygous Familial Hyperchole... More >>sterolemia Less << PHASE3 COMPLETED 2025-10-11 Cedars-Sinai Medical Center, L... More >>os Angeles, California, 90048, United States|University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|Robarts Research Institute, London, Ontario, N6A 5K8, Canada|Lipid Clinic and University of Montreal Community Genomic Medicine Center, Chicoutimi, Quebec, G7H 5H6, Canada|Dipartimento di Medicina Clinica e Della Patalogie Emergenti, Palermo, Sicily, Italy|Medicina Interna Universitaria, Ferrara, Italy|Centro Universitario Dislipidemie, Milano, Italy|Dipartimento di Clinica e Terapia Medica, Roma, Italy|Cardiology Research, Bloemfontein, 9300, South Africa|University of Capetown, Cape town, 7925, South Africa Less <<
NCT01760187 Healthy Volunteer Phase 1 Completed - United Kingdom ... More >> Richmond Pharmacology Ltd Croydon, Surrey, United Kingdom, CR7 7YE Less <<
NCT01556906 Homozygous Familial Hyperchole... More >>sterolemia Less << PHASE2 COMPLETED 2025-02-04 University of Pennsylvania, Ph... More >>iladelphia, Pennsylvania, 19104, United States Less <<
NCT01556906 Homozygous Familial Hyperchole... More >>sterolemia Less << PHASE2 COMPLETED 2025-02-04 University of Pennsylvania, Ph... More >>iladelphia, Pennsylvania, 19104, United States Less <<
NCT01915771 Intra-subject Variability of P... More >>harmacokinetics Less << Phase 1 Completed - United Kingdom ... More >> Richmond Pharmacology Croydon, Surrey, United Kingdom, CR7 7YE Less <<
NCT02399839 - Enrolling by invitation March 2028 -
NCT00359281 - Completed - -
NCT02080468 Healthy Phase 1 Completed - United States, Texas ... More >> Covance Clinical Research Unit, Inc Dallas, Texas, United States, 75247 Less <<
NCT00943306 Familial Hypercholesterolemia Phase 3 Completed - United States, California ... More >> Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Canada, Ontario Robarts Research Institute London, Ontario, Canada, N6A 5K8 Canada, Quebec Lipid Clinic and University of Montreal Community Genomic Medicine Center Chicoutimi, Quebec, Canada, G7H 5H6 Italy Medicina Interna Universitaria Ferrara, Sicily, Italy Dipartimento di Medicina Clinica e Delle Patologie Emergenti Palermo, Sicily, Italy Centro Universitario Dislipidemie Milano, Italy DAI Ematologia, Oncologia, Anatomia Patologica e Medicina Roma, Italy South Africa Cardiology Research Bloemfontein, South Africa, 9300 University of Capetown Cape town, South Africa, 7925 Less <<
NCT00943306 - Completed - -
NCT02135705 Homozygous Familial Hyperchole... More >>sterolemia Less << RECRUITING 2028-09-01 Brookwood Baptist Medical Cent... More >>er, Birmingham, Alabama, 35209, United States|Springhill Physician Practices, Mobile, Alabama, 36608, United States|Northern Arizona Healthcare, Cottonwood, Arizona, 86326, United States|One Medical, Gilbert, Arizona, 85296, United States|Scottsdale Family Health, Phoenix, Arizona, 85018, United States|Pima Heart, Tucson, Arizona, 85718, United States|Arkansas Heart Center, Fort Smith, Arkansas, 72901, United States|Cedars-Sinai Medical Center, Los Angeles, California, 90048, United States|University of Colorado Health, Aurora, Colorado, 80045, United States|Alfieri Cardiology, Newark, Delaware, 19713, United States|Preventative Cardiology, Inc., Boca Raton, Florida, 33434, United States|Florida Lipid Institute, Winter Park, Florida, 32792-2223, United States|Piedmont Heart Institute, Atlanta, Georgia, 30309, United States|Atlanta Heart Specialists, Cumming, Georgia, 30041, United States|Northside Hospital, Inc., Cumming, Georgia, 30041, United States|Comprehensive Cardiovascular Care, Gurnee, Illinois, 60031, United States|Community Health Network, Indianapolis, Indiana, 46250, United States|St. Vincent Medical Group, Inc., Indianapolis, Indiana, 46290, United States|Henry County Medical Center, New Castle, Kentucky, 40050, United States|Cardiovascular Institute of the South, Houma, Louisiana, 70360, United States|Get Well Immediate Care, Towson, Maryland, 21204, United States|University of Michigan Health System, Ann Arbor, Michigan, 48109, United States|Complete Family Care Cholesterol Treatment Center, Sterling Heights, Michigan, 48314, United States|Minneapolis Heart Institute Foundation, Minneapolis, Minnesota, 55407, United States|HealthEast Care System, Saint Paul, Minnesota, 55102, United States|Stern Cardiovascular Foundation, Southaven, Mississippi, 38671, United States|Methodist Physicians Clinic, Omaha, Nebraska, 68114, United States|Hackensack Meridian Health, Edison, New Jersey, 08817, United States|Avinash C. Gupta, MD, PC, Lakewood, New Jersey, 08701, United States|201 Route 17 North, Rutherford, New Jersey, 07070, United States|Valley Medical Group, Wyckoff, New Jersey, 07481, United States|Murray Hill Medical Group, New York, New York, 10016, United States|NY Heart Center, Syracuse, New York, 13210, United States|Pediatric Cardiology Associates, Syracuse, New York, 13210, United States|Cardiology Specialists of the Carolinas PA, Charlotte, North Carolina, 28204, United States|Cardiology Specialists Of Carolina, Charlotte, North Carolina, 28211, United States|The Heart Care Group, PC, Allentown, Pennsylvania, 18103, United States|St. Luke's University Health Network - Pennsylvania, Bethlehem, Pennsylvania, 18015, United States|Lehigh Valley Hospital And Health Network, East Stroudsburg, Pennsylvania, 18301, United States|Cardiology Consultants of Philadelphia, Philadelphia, Pennsylvania, 19107, United States|Thomas Jefferson University Health System, Philadelphia, Pennsylvania, 19148, United States|Palmetto Health, Columbia, South Carolina, 29203, United States|317 Saint Francis Dr., Greenville, South Carolina, 29601, United States|Cardiovascular Specialists of Texas, Austin, Texas, 78758, United States|Baylor Scott & White Health, Dallas, Texas, 75226, United States|The University of Vermont Health Network, Burlington, Vermont, 05401-1473, United States|West Virginia University Medicine, Morgantown, West Virginia, 26506, United States|Ascension, Milwaukee, Wisconsin, 53211, United States|Medical College of Wisconsin, Milwaukee, Wisconsin, 53226, United States|Aspirus Research Institute, Wausau, Wisconsin, 54401, United States|Clinica de Salud de Chaco, Reconquista, Chaco CPA, H3500BJS, Argentina|Nova Scotia Health Authority, Halifax, Nova Scotia, B3H2Y9, Canada|Robarts Research Institute, London, Ontario, N6A5B7, Canada|Ecogene-21, Chicoutimi, Quebec, G7H7K9, Canada|McGill University, Montréal, Quebec, H4A3J1, Canada|Centre Hospitalier Régional Universitaire de Lille, Lille, Cedex, 59037, France|Centre Hospitalier Universitaire Lyon, Bron, Lyon, 69677, France|Centre Hospitalier Universitaire Strasbourg, Strasbourg, 67000, France|University General Hospital of Ioannina, Ioánnina, 45500, Greece|Metropolitan Hospital, Piraeus, 18547, Greece|Policlinico S. Orsola-Malpighi, Bologna, BO, 40138, Italy|Azienda Ospedaliera G. Brotzu, Cagliari, CA, 09134, Italy|ASST Grande Ospedale Metropolitano Niguarda, Milano, MI, 20162, Italy|Azienda Ospedaliera Universitaria Policlinico Paolo Giaccone, Palermo, PA, 90127, Italy|Azienda Ospedaliera Universita di Padova, Padova, PD, 35128, Italy|Università degli Studi di Roma La Sapienza, Roma, RM, 00161, Italy|Università degli Studi di Roma La Sapienza, Roma, Rome, 00161, Italy|Azienda Ospedaliero-Universitaria San Luigi Gonzaga, Orbassano, TO, 10043, Italy|Azienda Ospedaliero Universi consorziale policlinico di Bari, Bari, 70120, Italy|Azienda Ospedaliera Specialistica Dei Colli, Napoli, 80131, Italy|Azienda Ospedaliera Universitaria Federico II, Napoli, 80131, Italy|CNR Regione Toscana - Fondazione Toscana Gabriele Monasterio, Pisa, 56124, Italy|Radboud Universiteit Medisch Centrum, Nijmegen, Gelderland, 6525 GA, Netherlands|Erasmus Medisch Centrum, Rotterdam, Zuid Holland, 3015 GD, Netherlands|Imperial College Healthcare - NHS Trust, London, W12 0NN, United Kingdom Less <<
NCT02765841 Homozygous Familial Hyperchole... More >>sterolemia Less << PHASE3 WITHDRAWN 2025-12-19 -
NCT02044419 Healthy Phase 1 Completed - United Kingdom ... More >> Richmond Pharmacology Ltd Croydon, Surrey, United Kingdom, CR7 7YE Less <<
NCT02044419 - Completed - -
NCT02399852 Homozygous Familial Hyperchole... More >>sterolemia Less << WITHDRAWN 2025-12-21 -
NCT01760187 - Completed - -
NCT02080455 Effect of Atorvastatin on the ... More >>Pharmacokinetics of Lomitapide Less << Phase 1 Completed - United States, Texas ... More >> Covance Clinical Research Unit, Inc Dallas, Texas, United States, 75247 Less <<
NCT02173158 - Completed - -
NCT02173158 Familial Hypercholesterolemia ... More >>- Homozygous Less << Phase 3 Completed - Japan ... More >> Kurume-shi, Fukuoka, Japan, 830-8522 Kanazawa, Ishikawa, Japan, 920-8641 Osakashi, Osaka, Japan, 530-00001 Suita-shi, Osaka, Japan, 565-8565 Tokorozawa, Saitama, Japan, 359-1142 Bunkyo-ku, Tokyo, Japan, 113-8519 Less <<
NCT04681170 Homozygous Familial Hyperchole... More >>sterolaemia (HoFH) Less << PHASE3 COMPLETED 2024-06-06 Universtiats-Kinderlinik Heide... More >>lberg, Heidelberg, Baden-Wurttemberg, 69120, Germany|University Hospital of Cologne, Cologne, 50937, Germany|University Medical Center Hamburg-Eppendorf, Hamburg, 20246, Germany|Chaim Sheba Medical Center, Ramat Gan,, 52621, Israel|U.O.C. Clinica Medica 1, Padova, Padua, 35128, Italy|Bambino Gesù Children's Hospital,, Roma, 00165, Italy|King Abdullah International Medical Research Centre (KAIMRC),, Riyadh, Saudi Arabia|King Faisal Specialist Hospital, Riyadh, Saudi Arabia|Hospital Universitari Sant Joan, Reus, Tarragona,, 43204, Spain|Hospital Abente y Lago, A Coru?a, 15006, Spain|Hospital Clinico Universitario of Valencia, Valencia, 46010, Spain|E.P.S. Fattouma Bourguiba Hospital, Monastir,, 5000, Tunisia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.44mL

0.29mL

0.14mL

7.21mL

1.44mL

0.72mL

14.42mL

2.88mL

1.44mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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