Lomitapide | Microsomal triglyceride transfer protein inhibitor

Lomitapide chemical structure Focus Biomolecules

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Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2  It has displayed anticancer activity acting through various pathways including autophagy-dependent cancer cell death via direct inhibition of the kinase activity of mTORC13, activation of AMPK/Beclin1-mediated autophagy4, Notch inhibition via targeting TACE and γ-secretase5, blocking ZDHHC5-dependent palmitoylation on SSTR56, PFKFB3 inhibition7, and PARP14/DRP1-mediated mitophagy8.

References/Citations:

  1. Wetterau et al. (1998), An MTP Inhibitor That Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits; Science 282 751
  2. Cuchel et al. (2013), Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolemia: a single-arm, open-label, phase 3 study; Lancet 381 40
  3. Lee et al. (2022), Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR; Cell Death Dis. 13 603
  4. Zuo et al. (2021), Targeting PP2A with lomitapide suppresses colorectal tumorigenesis through activation of AMPK/Beclin1-mediated autophagy; Cancer Lett. 521 281
  5. Sen et al. (2023), Multi-targeting TACE/ADAM17 and gamma-secretase of notch signaling pathway in TNBC via drug repurposing approach using Lomitapide; Cell Signal. 102 110529
  6. Wang et al. (2023), Repositioning Lomitapide to block ZDHHC5-dependent palmitoylation on SSTR5 leads to anti-proliferation effect in preclinical pancreatic cancer models; Cell Death Discov. 9 60
  7. Cao et al. (2024), Drug-repurposing by virtual and experimental screening of PFKFB3 inhibitors for pancreatic cancer therapy; Eur. J. Pharmacol. 965 176330
  8. Zhang et al. (2024), Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma; Cancer Lett. 588 216802
182431-12-5, AEGR-733, BMS-201038, Lomitapide, Lomitapide supplier, microsomal triglyceride transfer protein inhibitor, MTP inhibitor, MTTP inhibitor
Alternate Name:
AEGR-733; BMS-201038

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Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2  It has displayed anticancer activity acting through various pathways including autophagy-dependent cancer cell death via direct inhibition of the kinase activity of mTORC13, activation of AMPK/Beclin1-mediated autophagy4, Notch inhibition via targeting TACE and γ-secretase5, blocking ZDHHC5-dependent palmitoylation on SSTR56, PFKFB3 inhibition7, and PARP14/DRP1-mediated mitophagy8.

References/Citations:

  1. Wetterau et al. (1998), An MTP Inhibitor That Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits; Science 282 751
  2. Cuchel et al. (2013), Efficacy and safety of a microsomal triglyceride transfer protein inhibitor in patients with homozygous familial hypercholesterolemia: a single-arm, open-label, phase 3 study; Lancet 381 40
  3. Lee et al. (2022), Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR; Cell Death Dis. 13 603
  4. Zuo et al. (2021), Targeting PP2A with lomitapide suppresses colorectal tumorigenesis through activation of AMPK/Beclin1-mediated autophagy; Cancer Lett. 521 281
  5. Sen et al. (2023), Multi-targeting TACE/ADAM17 and gamma-secretase of notch signaling pathway in TNBC via drug repurposing approach using Lomitapide; Cell Signal. 102 110529
  6. Wang et al. (2023), Repositioning Lomitapide to block ZDHHC5-dependent palmitoylation on SSTR5 leads to anti-proliferation effect in preclinical pancreatic cancer models; Cell Death Discov. 9 60
  7. Cao et al. (2024), Drug-repurposing by virtual and experimental screening of PFKFB3 inhibitors for pancreatic cancer therapy; Eur. J. Pharmacol. 965 176330
  8. Zhang et al. (2024), Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma; Cancer Lett. 588 216802