Page last updated: 2024-12-06

colestipol

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Description

Colestipol is a non-absorbable bile acid sequestrant used to lower cholesterol levels in patients with high cholesterol. It is a synthetic polymer resin composed of quaternary ammonium groups attached to a polystyrene backbone. Colestipol works by binding to bile acids in the gut, preventing their reabsorption and promoting their excretion in feces. This leads to a reduction in the amount of cholesterol circulating in the blood. It is used to reduce the risk of heart disease and heart attacks in patients with high cholesterol. Colestipol is studied because it is a safe and effective way to lower cholesterol levels and reduce the risk of heart disease. It is also studied to understand its mechanisms of action and its potential side effects.'

Colestipol: Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

colestipol : A high molecular weight copolymer of diethylenetriamine and epichlorohydrin (hydrochloride), with approximately 1 out of 5 amine nitrogens protonated. Due to the highly cross-linked and insoluble nature of the material, no structural formula has been assigned and no specific molecular weight information is available. A basic anion exchange resin, it is used as its hydrochloride for binding bile acids in the intestine, inhibiting their reabsorption. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID62816
SCHEMBL ID1649962
MeSH IDM0004739

Synonyms (26)

Synonym
egalin
alseroxylon
rau-tab
rautensin
alseroxylon [jan]
rauwiloid
colestipol
C06925
26658-42-4
nsc147003
tetraethylenepentamine,3-epoxypropane
nsc-147003
u 26,597a
colestipolum [inn-latin]
u 26597a
50925-79-6
8001-95-4
SCHEMBL1649962
GMRWGQCZJGVHKL-UHFFFAOYSA-N
Q3294635
DTXSID00965206
n~1~,n~1'~-[azanediyldi(ethane-2,1-diyl)]di(ethane-1,2-diamine)--2-(chloromethyl)oxirane (1/1)
n1-(2-aminoethyl)-n2-(2-((2-aminoethyl)amino)ethyl)ethane-1,2-diamine compound with 2-(chloromethyl)oxirane (1:1)
n'-[2-[2-(2-aminoethylamino)ethylamino]ethyl]ethane-1,2-diamine;2-(chloromethyl)oxirane
AKOS040750357
PD010218

Research Excerpts

Overview

Colestipol is a safe, effective, cholesterol-lowering, bile-acid sequestrant that lowers low-density-lipoprotein (LDL) and total plasma cholesterol levels. It may prove to be very useful in the treatment of children heterozygous for familial hypercholesterolemia.

ExcerptReferenceRelevance
"Colestipol is an anion exchange resin with bile acid sequestering properties resembling those of cholestyramine, another lipid-lowering binding resin. "( Colestipol: a review of its pharmacological properties and therapeutic efficacy in patients with hypercholesterolaemia.
Avery, GS; Brogden, RN; Heel, RC; Pakes, GE; Speight, TM, 1980
)
3.15
"Colestipol is a safe, effective, cholesterol-lowering, bile-acid sequestrant that lowers low-density-lipoprotein (LDL) and total plasma cholesterol levels without consistently affecting high-density-lipoprotein (HDL) cholesterol levels. "( Colestipol and probucol: treatment of primary and familial hypercholesterolemia and amelioration of atherosclerosis.
Glueck, CJ, 1982
)
3.15
"Colestipol is an effective and well-tolerated cholesterol lowering compound which, in conjunction with diet, may prove to be very useful in the treatment of children heterozygous for familial hypercholesterolemia."( Pediatric familial type II hyperlipoproteinemia: therapy with diet and colestipol resin.
Fallat, RW; Glueck, CJ; Mellies, M; Tsang, RC, 1976
)
1.21
"Colestipol seems to be an effective and safe drug in the treatment of the famiial type II hyperlipoproteinemia, without escape phenonmenon."( Colestipol in familial type II hyperlipoproteinemia: a three-year trial.
Desager, JP; Harvengt, C, 1976
)
2.42
"Colestipol is an effective cholesterol (C)-lowering agent, but it must be taken in large doses and the palatability is poor. "( The effect of encapsulated, low-dose colestipol in patients with hyperlipidemia.
Demke, DM; Grzegorczyk, CR; Linet, OI, 1988
)
1.99

Actions

ExcerptReferenceRelevance
"Colestipol tended to increase serum triglyceride concentrations but the changes were not significant.(ABSTRACT TRUNCATED AT 250 WORDS)"( Colestipol at varying dosage intervals in the treatment of moderate hypercholesterolaemia.
Fowler, G; Lyons, D; Petrie, JC; Webster, J, 1994
)
2.45

Treatment

Colestipol hydrochloride treatment significantly reduced both serum and arterial total cholesterol levels by 50 and 59%, respectively. Treatment produced a disproportionate decrease in LDL cholesterol compared to LDL apoB, resulting in a significant decrease in the LDL cholesterol/apoB ratio.

ExcerptReferenceRelevance
"Colestipol treatment was not associated with any significant change in HDL cholesterol levels and minor increases in triglycerides."( Effect of colestipol and clofibrate on plasma lipid and lipoproteins in type IIa hyperlipoproteinemia.
Crow, LO; Hunninghake, DB; Isaacson, SO; Probstfield, JL, 1981
)
1.39
"Colestipol treatment was found to be bioequivalent to the control treatment by Schuirmann's two one-sided t tests, while cholestyramine treatment was found to be bioinequivalent.(ABSTRACT TRUNCATED AT 250 WORDS)"( The effect of colestipol and cholestyramine on ibuprofen bioavailability in man.
al-Balla, SR; al-Meshal, MA; el-Sayed, YM; Gouda, MW, 1994
)
1.37
"Colestipol treatment did not change these parameters."( The effect of colestipol and cholestyramine on the systemic clearance of intravenous ibuprofen in rabbits.
al-Angary, AA; al-Meshal, MA; el-Sayed, YM; Gouda, MW; Lutfi, KM, 1994
)
1.37
"Colestipol hydrochloride treatment significantly reduced both serum and arterial total cholesterol levels by 50 and 59%, respectively."( Anti-atherosclerotic activity of colestipol hydrochloride in SEA quail.
Day, CE, 1990
)
1.28
"Colestipol treatment produced a disproportionate decrease in LDL cholesterol compared to LDL apoB, resulting in a significant decrease in the LDL cholesterol/apoB ratio."( Colestipol-induced changes in LDL composition and metabolism. II. Studies in humans.
Carew, TE; Krauss, RW; Lindgren, FT; Witztum, JL; Young, SG, 1989
)
2.44
"Treatment with colestipol tablets and colestipol granules resulted in virtually identical, statistically significant (P < or = 0.05) reductions of LDL-C, total cholesterol (TC), TC/HDL-C, and apolipoprotein B (apo B)."( The effects of colestipol tablets compared with colestipol granules on plasma cholesterol and other lipids in moderately hypercholesterolemic patients.
Davidson, MH; Demke, DM; Dujovne, CA; Eckert, SM; Ginsberg, D; Goldberg, AC; Hodis, HN; Hughes, TA; Insull, W; Kane, JP, 1995
)
0.98

Toxicity

ExcerptReferenceRelevance
" However, case reports and pharmacokinetic data disclose 3 kinds of adverse effects: (1) the decreased absorption of concomitant medications and sometimes of certain vitamins; (2) the physicochemical alteration of intestinal contents leading to constipation and, very rarely, intestinal obstruction; and (3) modest increases in plasma triglyceride levels due to the alteration of hepatic lipid metabolism."( Safety considerations with gastrointestinally active lipid-lowering drugs.
Armani, A; Guyton, JR; Jacobson, TA; McKenney, JM, 2007
)
0.34

Pharmacokinetics

The effect of oral administration of the non-absorbable anion-exchange resins cholestyramine and colestipol on the systemic clearance and other pharmacokinetic parameters of ibuprofen (25 mg kg-1) was studied in rabbits.

ExcerptReferenceRelevance
" After concomitant single-dose administration, the serum p-chlorophenoxyisobutyric acid levels, bioavailability parameters, and pharmacokinetic parameters investigated provided no evidence for an interaction and suggested that colestipol and clofibrate can be administered concomitantly or at separated in tervals according to whichever dosage regimen is deemed advisable by the physician."( The effect of colestipol hydrochloride on the bioavailability and pharmacokinetics of clofibrate.
Albert, KS; DeSante, KA; DiSanto, AR; Vecchio, TJ; Weber, DJ; Welch, RD,
)
0.68
"The possibility of a pharmacokinetic interaction between two hypolipidemic drugs, colestipol, an ion exchange resin, and fenofibrate, a phenoxyacid derivative, was studied in 6 male volunteers."( Lack of pharmacokinetic interaction of colestipol and fenofibrate in volunteers.
Desager, JP; Harvengt, C, 1980
)
0.76
"The effect of oral administration of the non-absorbable anion-exchange resins cholestyramine and colestipol on the systemic clearance and other pharmacokinetic parameters of intravenously administered ibuprofen (25 mg kg-1) was studied in rabbits."( The effect of colestipol and cholestyramine on the systemic clearance of intravenous ibuprofen in rabbits.
al-Angary, AA; al-Meshal, MA; el-Sayed, YM; Gouda, MW; Lutfi, KM, 1994
)
0.87

Compound-Compound Interactions

The effects of colestipol therapy alone (20 g/d. or combined with simvastatin (20 mg/d) were examined in a group of eight male patients with primary moderate hypercholesterolemia.

ExcerptReferenceRelevance
" However, when colestipol was given with gemfibrozil, there was a decrease in AUC (43."( Apparent reduced absorption of gemfibrozil when given with colestipol.
Cutler, RE; Feng, Y; Forland, SC, 1990
)
0.88
"Recent trials have investigated the usefulness of fenofibrate, alone and in combination with other lipid-lowering therapies, in the treatment of hyperlipidemia."( Review of clinical studies of fenofibrate in combination with currently approved lipid-lowering drugs.
Brown, WV, 1989
)
0.28
" Fibrates also have the potential to cause rhabdomyolysis, although generally only in combination with HMG-CoA reductase inhibitors, and are subject to binding by concomitantly administered bile acid sequestrants."( Antihyperlipidaemic agents. Drug interactions of clinical significance.
Farmer, JA; Gotto, AM, 1994
)
0.29
" Following an 8-week dietary phase, participants were randomized to treatment with 20 mg of lovastatin combined with 5 g or with 10 g of colestipol, or to matching placebo."( Effectiveness of low-dose lovastatin combined with low-dose colestipol in moderate to severe primary hypercholesterolaemia.
de Koning Gans, HJ; Gørbitz, C; Harrison, EM; Ose, L; Tonstad, S, 1993
)
0.73

Bioavailability

The purpose of this study was to determine whether a concomitant single oral dose of one of the anion exchange resins colestipol hydrochloride (10 g) or cholestyramine (8 g) administered with ibuprofen (400 mg) would alter the bioavailability of this non-steroidal anti-inflammatory agent. The data suggest a reduction of gemfibrozil bioavailability when colstipol is administered concomitantly.

ExcerptReferenceRelevance
" After concomitant single-dose administration, the serum p-chlorophenoxyisobutyric acid levels, bioavailability parameters, and pharmacokinetic parameters investigated provided no evidence for an interaction and suggested that colestipol and clofibrate can be administered concomitantly or at separated in tervals according to whichever dosage regimen is deemed advisable by the physician."( The effect of colestipol hydrochloride on the bioavailability and pharmacokinetics of clofibrate.
Albert, KS; DeSante, KA; DiSanto, AR; Vecchio, TJ; Weber, DJ; Welch, RD,
)
0.68
" Applications are given to a comparative bioavailability trial for attainment of steady state levels and to a clinical trial to compare the effects of two hypolipidemics."( The analysis of the two-period repeated measurements crossover design with application to clinical trials.
Fisher, AC; Wallenstein, S, 1977
)
0.26
" The data suggest a reduction of gemfibrozil bioavailability when colestipol is administered concomitantly."( Apparent reduced absorption of gemfibrozil when given with colestipol.
Cutler, RE; Feng, Y; Forland, SC, 1990
)
0.76
" The bioavailability was reduced by colestipol 80%, by cholestyramine 95% and by activated charcoal 99."( Effects of resins and activated charcoal on the absorption of digoxin, carbamazepine and frusemide.
Hirvisalo, EL; Kivistö, K; Neuvonen, PJ, 1988
)
0.55
" Bile acid sequestrants are the most difficult of these agents to administer concomitantly, because their nonspecific binding results in decreased bioavailability of a number of other drugs, including thiazide diuretics, digitalis preparations, beta-blockers, coumarin anticoagulants, thyroid hormones, fibric acid derivatives and certain oral antihyperglycaemia agents."( Antihyperlipidaemic agents. Drug interactions of clinical significance.
Farmer, JA; Gotto, AM, 1994
)
0.29
" The in-vivo data suggest a reduction of diclofenac bioavailability when colestipol or cholestyramine is administered concomitantly."( The effects of cholestyramine and colestipol on the absorption of diclofenac in man.
al-Balla, SR; al-Meshal, MA; el-Sayed, YM; Gouda, MW, 1994
)
0.8
"The purpose of this study was to determine whether a concomitant single oral dose of one of the anion exchange resins colestipol hydrochloride (10 g) or cholestyramine (8 g) administered with ibuprofen (400 mg) would alter the bioavailability of this non-steroidal anti-inflammatory agent."( The effect of colestipol and cholestyramine on ibuprofen bioavailability in man.
al-Balla, SR; al-Meshal, MA; el-Sayed, YM; Gouda, MW, 1994
)
0.86
" An illustration of the application of the program is presented to compare the bioavailability of ibuprofen when administered alone or followed by colestipol hydrochloride or by cholestyramine."( Design of crossover microcomputer program and application on drug bioequivalence data.
Abdullah, ME; El-Sayed, YM, 1995
)
0.49

Dosage Studied

A dose-response study was performed with three doses of colestipol to assess bile acid sequestering activity in 40 volunteers. The effect was most prominent in the high dosage (75 mg per kg per day) candicidin group. Although it did not completely eliminate teriflunomide with the same effectiveness as cholestyramine, it may offer an alternative method for accelerated elimination of terifnomide.

ExcerptRelevanceReference
" The effect was most prominent in the high dosage (75 mg per kg per day) candicidin group and moderate in the high dosage (400 mg per kg per day) colestipol group."( Effect of candicidin and colestipol on the testes and prostate glands of BIO 87.20 hamsters.
Schaffner, CP; Wang, GM, 1976
)
0.76
" After concomitant single-dose administration, the serum p-chlorophenoxyisobutyric acid levels, bioavailability parameters, and pharmacokinetic parameters investigated provided no evidence for an interaction and suggested that colestipol and clofibrate can be administered concomitantly or at separated in tervals according to whichever dosage regimen is deemed advisable by the physician."( The effect of colestipol hydrochloride on the bioavailability and pharmacokinetics of clofibrate.
Albert, KS; DeSante, KA; DiSanto, AR; Vecchio, TJ; Weber, DJ; Welch, RD,
)
0.68
"Subjects were randomly assigned to receive either colestipol placebo or colestipol 5 g or 10 g each morning in fixed dosage for 18 weeks."( Successful management of primary hypercholesterolaemia with simvastatin and low-dose colestipol.
Parfitt, A; Simons, J; Simons, LA, 1992
)
0.76
" Such combination therapy offers the possibility of improved cholesterol lowering without the need for full dosage of either drug."( Successful management of primary hypercholesterolaemia with simvastatin and low-dose colestipol.
Parfitt, A; Simons, J; Simons, LA, 1992
)
0.51
" This retrospective data analysis suggests that the combination of gemfibrozil and lovastatin may be safe in patients with normal renal function when the dosage of lovastatin is limited and when CK and ALT levels are monitored carefully."( A retrospective review of the use of lipid-lowering agents in combination, specifically, gemfibrozil and lovastatin.
McIntyre, TH; Shapiro, ML; Whitney, EJ; Wirebaugh, SR, 1992
)
0.28
" This original design allowed to define the most appropriate individual cholesterol-lowering drug dosage in FH patients."( Lecithin: cholesterol acyltransferase activity in familial hypercholesterolemia treated with simvastatin and simvastatin plus low-dose colestipol.
Desager, JP; Harvengt, C; Horsmans, Y, 1991
)
0.48
"A dose-response study was performed with three doses of colestipol, using postprandial serum bile acid levels to assess bile acid sequestering activity in 40 volunteers with asymptomatic hyperlipidaemia."( The effect of colestipol dose on postprandial serum bile acid concentration: assessment by an enzymic bioluminescence procedure.
Angellotti, MA; Daei, F; Fleishaker, JC; Hofmann, AF; Rossi, SS; Smith, RB; Welshman, IR, 1990
)
0.89
" In particular, modest lowering of dosage may preserve considerable LDL cholesterol lowering and virtually eliminate side effects."( Review of clinical studies of bile acid sequestrants for lowering plasma lipid levels.
LaRosa, J, 1989
)
0.28
"5% in the diet in combination with feed restriction was not consistently effective in removing body burdens of PBB from chickens previously fed 1 or 10 ppm PBBs, indicating a dose-response effect."( Procedures to enhance withdrawal of xenobiotics from chickens.
Bursian, S; Leavitt, R; Lehning, E; Polin, D; Pullen, D, 1985
)
0.27
" Each patient usually received more than one of the four dosage intervals."( The effect of encapsulated, low-dose colestipol in patients with hyperlipidemia.
Demke, DM; Grzegorczyk, CR; Linet, OI, 1988
)
0.55
" As with cholestyramine, colestipol may bind with other concomitantly administered drugs reducing their absorption or enterohepatic recirculation; dosage intervals of other concurrent medications should be adjusted to minimise the potential for such an interaction."( Colestipol: a review of its pharmacological properties and therapeutic efficacy in patients with hypercholesterolaemia.
Avery, GS; Brogden, RN; Heel, RC; Pakes, GE; Speight, TM, 1980
)
2.01
" We have investigated a low dosage regimen with varying dosage intervals in order to assess efficacy and tolerability."( Colestipol at varying dosage intervals in the treatment of moderate hypercholesterolaemia.
Fowler, G; Lyons, D; Petrie, JC; Webster, J, 1994
)
1.73
" As adjunctive COL treatment in hyperthyroidism allows reducing MMI dosage it may decrease the rate of dose dependent MMI side effects."( Role of colestipol in the treatment of hyperthyroidism.
Hagag, P; Nissenbaum, H; Weiss, M, 1998
)
0.73
" In contrast, Carbosorb AC did not affect the AUC,yet increased Tmax In another study, mortality was assessed 96 h after rats were orally dosed with 5 mg FA/kg followed by gavage with 2 g/kg Carbosorb AC, colestipol or water immediatey or 30 min after dosing."( Sorption of fluoroacetate (compound 1080) by Colestipol, activated charcoal and anion-exchange in resins in vitro and gastrointestinal decontamination in rats.
Ataria, J; Eason, CT; Norris, WR; Temple, WA; Wickstrom, ML; Wright, GR, 2000
)
0.75
"The pharmacology, pharmacodynamics, clinical efficacy, drug interactions, adverse effects, and dosage and administration of colesevelam hydrochloride are reviewed."( Colesevelam hydrochloride.
Steinmetz, KL, 2002
)
0.31
" Results from these two studies show that colestipol can cause a significant decrease in diltiazem absorption from both IR and SR dosage forms."( Effect of concomitant colestipol hydrochloride administration on the bioavailability of diltiazem from immediate- and sustained-release formulations.
Jungbluth, GL; Knuth, DW; Turner, SW, 2002
)
0.89
" Currently, AEPs with oral cholestyramine or activated charcoal are available but are restricted by adverse effects, limited administration routes, and dosing frequencies."( Tolerability and efficacy of colestipol hydrochloride for accelerated elimination of teriflunomide.
Aungst, A; Casady, L; Dixon, C; Maldonado, J; McCoy, B; Moreo, N; Robertson, D, 2017
)
0.75
" Although colestipol HCl did not completely eliminate teriflunomide with the same effectiveness as cholestyramine, it may offer an alternative method for accelerated elimination of teriflunomide with potentially improved tolerability and more favorable dosing and administration options."( Tolerability and efficacy of colestipol hydrochloride for accelerated elimination of teriflunomide.
Aungst, A; Casady, L; Dixon, C; Maldonado, J; McCoy, B; Moreo, N; Robertson, D, 2017
)
1.15
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (373)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990214 (57.37)18.7374
1990's113 (30.29)18.2507
2000's30 (8.04)29.6817
2010's13 (3.49)24.3611
2020's3 (0.80)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 92.06

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index92.06 (24.57)
Research Supply Index6.23 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index166.95 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (92.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials110 (27.57%)5.53%
Reviews52 (13.03%)6.00%
Case Studies15 (3.76%)4.05%
Observational2 (0.50%)0.25%
Other220 (55.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Prospective, Open Label Comparison of Ezetimibe, Niacin, and Colestipol as Adjunct Therapy in Lipid Reduction [NCT00203476]Phase 430 participants (Actual)Interventional2005-05-31Completed
Familial Atherosclerosis Treatment Study [NCT00000512]Phase 3146 participants (Actual)Interventional1984-01-31Completed
[NCT00000599]Phase 30 participants Interventional1980-06-30Completed
An Open-Label Study to Characterize the Incidence and Severity of Diarrhea in Patients With Early-Stage HER2+ Breast Cancer Treated With Neratinib and Loperamide [NCT02400476]Phase 2563 participants (Actual)Interventional2015-02-28Completed
Sorbent Therapy of the Cutaneous Porphyrias [NCT01422915]Phase 2/Phase 34 participants (Actual)Interventional2011-05-31Completed
Rapid Elimination Procedure of Teriflunomide With Colestipol Hydrochloride [NCT02263547]Phase 114 participants (Actual)Interventional2015-03-31Terminated(stopped due to PK time points were not being met as expected. Determination that risks outweighed benefit.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00203476 (4) [back to overview]Incidents of Rhabdomyolysis
NCT00203476 (4) [back to overview]LDL Goal Attainment
NCT00203476 (4) [back to overview]LFT Elevation
NCT00203476 (4) [back to overview]Change in HDL From Baseline to 12 Weeks.
NCT01422915 (2) [back to overview]Photosensitivity, Assessed by Measuring the Number of Minutes of Sun Tolerance
NCT01422915 (2) [back to overview]Protoporphyrin Concentration in Blood
NCT02263547 (2) [back to overview]Primary Outcome Measures: Teriflunomide Concentrations at Day 28
NCT02263547 (2) [back to overview]Secondary Outcome Measure: Mean Percentage Change of Serum Teriflunomide Levels Percentage Change of Teriflunomide Concentrations at Day 8, Day 14, Day 26 ad Day 36 Following Administration of Colestipol Hydrochloride Tablets.
NCT02400476 (3) [back to overview]Percentage of Patients With Grade 3 or Higher Diarrhea, According to NCI CTCAE v4.0.
NCT02400476 (3) [back to overview]Percentage of Patients With Diarrhea by Grade, According to the National Cancer Institute Common Terminology Criteria (NCI CTCAE), Version 4.0.
NCT02400476 (3) [back to overview]Percentage of Patients With Serious Adverse Events and Other Adverse Events of Special Interest

Incidents of Rhabdomyolysis

(NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin0
Colestipol0
Ezetimibe0

[back to top]

LDL Goal Attainment

Each participant had his LDL goal calculated based on the NCEP ATPIII guidelines. (NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin6
Colestipol6
Ezetimibe9

[back to top]

LFT Elevation

(NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin1
Colestipol1
Ezetimibe2

[back to top]

Change in HDL From Baseline to 12 Weeks.

(NCT00203476)
Timeframe: baseline and 12 weeks

,,
Interventionmg/dl (Mean)
baseline12 weeks
Colestipol39.2237.56
Ezetimibe32.9034.70
Niacin42.3343.00

[back to top]

Photosensitivity, Assessed by Measuring the Number of Minutes of Sun Tolerance

Minutes of sun tolerance (NCT01422915)
Timeframe: At 60 days of treatment

Interventionminutes (Mean)
Colestipol Treatment65.8

[back to top]

Protoporphyrin Concentration in Blood

"erythrocyte protoporphyrin concentration, ug/dl~plasma protoporphyrin concentration, ug/dl" (NCT01422915)
Timeframe: Samples collected while on treatment (range 93-208 treatment days)

Interventionug/dl (Mean)
Erythrocyte ProtoporphyrinPlasma Protoporphyrin
Colestipol Treatment17125.8

[back to top]

Primary Outcome Measures: Teriflunomide Concentrations at Day 28

After receiving 14 days of teriflunomide, participants will take 11 days of colestipol to wash out the teriflunomide (measuring the levels of teriflunomide in the blood at each visit) (NCT02263547)
Timeframe: 28 days after the start in the study

Interventionteriflunomide level (mcg/ml) (Mean)
Teriflunomide Elimination With Colestipol9.36

[back to top]

Secondary Outcome Measure: Mean Percentage Change of Serum Teriflunomide Levels Percentage Change of Teriflunomide Concentrations at Day 8, Day 14, Day 26 ad Day 36 Following Administration of Colestipol Hydrochloride Tablets.

The last blood draw will be about 50 days from the start of the study (NCT02263547)
Timeframe: duration of study about 50 days

Interventionpercentage change in teriflunomide level (Mean)
8 days after colestipol hcl administered14 days after colestipol hcl administered26 days after colestipol hcl administered36 days after colestipol hcl administered
Teriflunomide Elimination With Colestipol-56.4-74.9-94.9-96.9

[back to top]

Percentage of Patients With Grade 3 or Higher Diarrhea, According to NCI CTCAE v4.0.

The primary objective of this study is to characterize the percentage of patients with Grade 3 or higher diarrhea in patients with early-stage HER2 overexpressed/amplified (HER2+) breast cancer treated with neratinib when administered with intensive loperamide prophylaxis, after prior treatment with trastuzumab. Grade 3: Increase of >=7 stools per day over baseline; incontinence; hospitalization indicated; severe increase in ostomy output compared to baseline; limiting self care ADL. Grade 4: Life-threatening consequences; urgent intervention indicated. Grade 5: Death. (NCT02400476)
Timeframe: From first dose of investigational product through 28 days after last dose, up to 15.5 months.

InterventionPercentage of participants (Number)
Loperamide30.7
Budesonide and Loperamide28.1
Colestipol and Loperamide20.6
Colestipol With Loperamide as Needed32.7
Neratinib Dose Escalation 113.3
Neratinib Dose Escalation 227.4

[back to top]

Percentage of Patients With Diarrhea by Grade, According to the National Cancer Institute Common Terminology Criteria (NCI CTCAE), Version 4.0.

Assess the percentage of patients with diarrhea after the administration of an anti-inflammatory agent, a bile acid sequestrant, or following two different dose-escalation regimens of neratinib, by maximum CTC grade. Grade 1: an increase of <4 stools per day over baseline; mild increase in ostomy output compared to baseline. Grade 2: Increase of 4 - 6 stools per day over baseline; moderate increase in ostomy output compared to baseline. Grade 3: Increase of >=7 stools per day over baseline; incontinence; hospitalization indicated; severe increase in ostomy output compared to baseline; limiting self care ADL. Grade 4: Life-threatening consequences; urgent intervention indicated. Grade 5: Death. (NCT02400476)
Timeframe: From first dose of investigational product through 28 days after last dose, up to 15.5 months.

,,,,,
InterventionPercentage of participants (Number)
Percentage of Patients w Grade 1 DiarrheaPercentage of Patients w Grade 2 DiarrheaPercentage of Patients w Grade 3 Diarrhea
Budesonide and Loperamide23.434.428.1
Colestipol and Loperamide27.934.620.6
Colestipol With Loperamide as Needed32.729.832.7
Loperamide24.124.830.7
Neratinib Dose Escalation 140.045.013.3
Neratinib Dose Escalation 237.133.927.4

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Percentage of Patients With Serious Adverse Events and Other Adverse Events of Special Interest

Assess the percentage of patients with serious adverse events (SAEs) and other adverse events of special interest (AESI). AESIs were selected based on the known safety profile of neratinib as well as typical key body system toxicity concerns generally reviewed for any new drug. These AESIs were grouped into the following categories: gastrointestinal toxicity (diarrhea and stomatitis), hepatotoxicity, pulmonary toxicity (interstitial lung disease), cardiac toxicity (LVEF decreased), and dermatologic toxicity (rash and nail disorders). The AESIs were analyzed by searching the clinical database for all TEAEs and SAEs using either Standardized MedDRA Queries (SMQs) or, if an applicable SMQ did not exist, a Sponsor-defined list of MedDRA preferred terms. (NCT02400476)
Timeframe: From first dose of investigational product through 28 days after last dose, up to 15.5 months.

,,,,,
Interventionpercentage of participants (Number)
Percentage of Patients with SAEsPercentage of Patients with AESI-Gastrointestinal Toxicities (Diarrhoea and Stomatitis Broad Search)Percentage of Patients with-Hepatotoxicities SMQ (Broad Search)Percentage of Patients with AESI- Interstitial Lung Disease SMQ (Broad Search)Percentage of Patients with AESI-Cardiac Toxicities SMQ (Broad Search)Percentage of Patients with AESI - Dermatologic Toxicities (Rash and Nail Disorders)Percentage of Patients with AESI-Gastrointestinal Toxicities (Narrow Search)Percentage of Patients with AESI-Hepatotoxicities SMQ (Narrow Search)Percentage of Patients with AESI- Interstitial Lung Disease SMQ (Narrow Search)Percentage of Patients with AESI-Cardiac Toxicities SMQ (Narrow Search)
Budesonide and Loperamide6.2587.57.8106.2537.5085.947.8100
Colestipol and Loperamide6.6283.824.41010.2923.5383.093.6801.47
Colestipol With Loperamide as Needed2.8896.154.8107.6918.2795.193.8500.96
Loperamide6.5781.7512.4105.8412.4180.2910.9502.92
Neratinib Dose Escalation 18.3398.338.33010.0011.6798.338.3301.67
Neratinib Dose Escalation 28.0698.394.8404.8430.6598.394.8400

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