Clinical experience with R103757, a potent inhibitor of microsomal triglyceride transfer protein (MTP)

Dupont, Alain; Cree, J. De; Vermeulen, Royce; Salvo, W.; Deridder, F.

doi:10.1016/s0021-9150(99)80147-6

Cited by 4 publications

(4 citation statements)

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“…An initial evaluation of the physicochemical characteristics of the drug suggested that oral bioavailability for R103757 was likely to be poor. This was based on the very low aqueous solubility and the estimated effective human dose, which was approximately 1 mg/kg (or 100 mg) 1. To confirm this assumption, a proof of principle study was completed in male beagle dogs using three different formulations.…”

Section: Resultsmentioning

confidence: 99%

“…Inhibiting MTP, therefore, blocks the formation of very low density lipoproteins and low density lipoproteins by the liver and of chylomicrons by the gut. Because chylomicrons carry dietary lipids from the gut to the liver, inhibition of the formation of these structures will prevent the uptake of lipids and may therefore be of use in the treatment of obesity 1,2. One potent MTP inhibitor that has been identified is R103757, a product of Johnson & Johnson Pharmaceutical Research and Development.…”

Section: Introductionmentioning

confidence: 99%

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Review of Preoperative Magnetic Resonance Imaging (MRI) in Breast Cancer: Should MRI Be Performed on All Women with Newly Diagnosed, Early Stage Breast Cancer?

Houssami¹,

Hayes²

2009

CA: A Cancer Journal for Clinicians

239

145

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Randomized controlled trials have shown equivalent survival for women with early stage breast cancer who are treated with breast-conservation therapy (local excision and radiotherapy) or mastectomy. Decades of experience have demonstrated that breast-conservation therapy provides excellent local control based on defined standards of care. Magnetic resonance imaging (MRI) has been introduced in preoperative staging of the affected breast in women with newly diagnosed breast cancer because it detects additional foci of cancer that are occult on conventional imaging. The median incremental (additional) detection for MRI has been estimated as 16% in meta-analysis. In the absence of consensus on the role of preoperative MRI, we review data on its detection capability and its impact on treatment. We outline that the assumptions behind the adoption of MRI, namely that it will improve surgical planning and will lead to a reduction in re-excision surgery and in local recurrences, have not been substantiated by trials. Evidence consistently shows that MRI changes surgical management, usually from breast conservation to more radical surgery; however, there is no evidence that it improves surgical care or prognosis. Emerging data indicate that MRI does not reduce re-excision rates and that it causes false positives in terms of detection and unnecessary surgery; overall there is little high-quality evidence at present to support the routine use of preoperative MRI. Randomized controlled trials are needed to establish the clinical, psychosocial, and long-term effects of MRI and to show a related change in treatment from standard care in women newly affected by breast cancer.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Review of Preoperative Magnetic Resonance Imaging (MRI) in Breast Cancer: Should MRI Be Performed on All Women with Newly Diagnosed, Early Stage Breast Cancer?

Houssami¹,

Hayes²

2009

CA: A Cancer Journal for Clinicians

239

145

View full text Add to dashboard Cite

show abstract

“…This was based on the very low aqueous solubility and the estimated effective human dose, which was approximately 1 mg/kg (or 100 mg). 1 To confirm this assumption, a proof of principle study was completed in male beagle dogs using three different formulations. The first dosage form was a fast-disintegrating tablet containing the crystalline drug substance (50-mg crystalline drug tablet).…”

Section: Resultsmentioning

confidence: 99%

“…Because chylomicrons carry dietary lipids from the gut to the liver, inhibition of the formation of these structures will prevent the uptake of lipids and may therefore be of use in the treatment of obesity. 1,2 One potent MTP inhibitor that has been identified is R103757, a product of Johnson & Johnson Pharmaceutical Research and Development.…”

Section: Introductionmentioning

confidence: 99%

The use of three different solid dispersion formulations—melt extrusion, film-coated beads, and a glass thermoplastic system—to improve the bioavailability of a novel microsomal triglyceride transfer protein inhibitor

Verreck¹,

Vandecruys²,

Conde³

et al. 2004

Journal of Pharmaceutical Sciences

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Dyslipidemia

2006

Wiley Handbook of Current and Emerging Drug Therapies

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Clinical experience with R103757, a potent inhibitor of microsomal triglyceride transfer protein (MTP)

Cited by 4 publications

References 0 publications

Review of Preoperative Magnetic Resonance Imaging (MRI) in Breast Cancer: Should MRI Be Performed on All Women with Newly Diagnosed, Early Stage Breast Cancer?

Review of Preoperative Magnetic Resonance Imaging (MRI) in Breast Cancer: Should MRI Be Performed on All Women with Newly Diagnosed, Early Stage Breast Cancer?

The use of three different solid dispersion formulations—melt extrusion, film-coated beads, and a glass thermoplastic system—to improve the bioavailability of a novel microsomal triglyceride transfer protein inhibitor

Dyslipidemia

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