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US Approved Rx

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Primary Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase

6

Cytochrome P450 3A4

6

HMG-CoA reductase

6

Solute carrier organic anion transporter family member 1B1

6

Solute carrier organic anion transporter family member 3A1

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1994

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Unknown

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Coronary heart disease mortality and cardiovascular events

6

Homozygous and heterozygous familial hypercholesterolemia

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Hyperlipidemia

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Atopic dermatitis

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ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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ATC Level 4

Calcineurin inhibitors

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Showing 1 - 9 of 9 results

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TACROLIMUS ANHYDROUS

Y5L2157C4J

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Status:

US Approved Rx (2025)

First approved in 1994

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

FK506-binding protein 1A

Conditions:

Organ rejection

Atopic dermatitis

Tacrolimus, previously known as FK506, is the active ingredient in Prograf. Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506...

binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription. Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action is not known. Experimental evidence suggests that tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin inhibited. This effect may prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). The net result is the inhibition of T-lymphocyte activation (i.e., immunosuppression). Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver transplants, kidney transplants, heart transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.

TENIVASTATIN

9L6M5TH46B

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

STATINE

YTC77XR1EK

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

TACROLIMUS

WM0HAQ4WNM

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Status:

US Approved Rx (2025)

First approved in 1994

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

FK506-binding protein 1A

Conditions:

Organ rejection

Atopic dermatitis

Tacrolimus, previously known as FK506, is the active ingredient in Prograf. Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506...

binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription. Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action is not known. Experimental evidence suggests that tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin inhibited. This effect may prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). The net result is the inhibition of T-lymphocyte activation (i.e., immunosuppression). Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver transplants, kidney transplants, heart transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.

SIMVASTATIN

AGG2FN16EV

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

TENIVASTATIN SODIUM

2L6JSY5YGL

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

TENIVASTATIN AMMONIUM

76RD797JAX

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

TENIVASTATIN CALCIUM

YNO268EI8T

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

TENIVASTATIN CALCIUM HYDRATE

QSL5L73L0O

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Status:

US Approved Rx (2016)

First approved in 1991

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Solute carrier organic anion transporter family member 3A1

Solute carrier organic anion transporter family member 1B1

3-hydroxy-3-methylglutaryl-coenzyme A reductase

Cytochrome P450 3A4

HMG-CoA reductase

Conditions:

Coronary heart disease mortality and cardiovascular events

Homozygous and heterozygous familial hypercholesterolemia

Simvastatin is a HMG-CoA Reductase Inhibitor that is FDA approved for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. It reduces levels of "bad" cholesterol (low-de...

nsity lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL). Common adverse reactions include abdominal pain, constipation, nausea, headache, upper respiratory infection. Cases of myopathy/rhabdomyolysis have been observed with simvastatin co-administered with lipid-modifying doses ( ≥ 1 g/day niacin) of niacin-containing products. The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of amiodarone, dronedarone, ranolazine, or calcium channel blockers such as verapamil, diltiazem, or amlodipine.

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