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US Approved Rx

23

Possibly Marketed Outside US

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Glucocorticoid receptor

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FK506-binding protein 1A

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1991

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1994

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Acne rosacea

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Allergic conjunctivitis

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Bacterial conjunctivitis

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Merck Sharp & Dohme

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ATC Level 1

DERMATOLOGICALS

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Calcineurin inhibitors

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Showing 1 - 10 of 24 results

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TACROLIMUS ANHYDROUS

Y5L2157C4J

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Status:

US Approved Rx (1994)

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.

DEXAMETHASONE

7S5I7G3JQL

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

2-HYDROXYETHYL METHACRYLATE

6E1I4IV47V

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Status:

Possibly Marketed Outside US

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

TACROLIMUS

WM0HAQ4WNM

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Status:

US Approved Rx (1994)

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.

Dexamethasone 21-sulfate

VMN9Z37FQR

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

DEXAMETHASONE SODIUM SUCCINATE

UZA9VMT64W

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

DEXAMETHASONE SUCCINATE

9UY5TBO121

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

DEXAMETHASONE 21-VALERATE

F2EHP3G50P

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

DEXAMETHASONE SODIUM SULFATE

41B47ECP9F

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

DEXAMETHASONE METASULFOBENZOATE

C67221CB9Q

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Status:

US Approved Rx (2020)

First approved in 1958

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Glucocorticoid receptor

Glucocorticoid receptor

Mineralocorticoid receptor

Conditions:

Herpes zoster keratitis

Allergic conjunctivitis

Superficial punctate keratitis

Bacterial conjunctivitis

Multiple myeloma

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune respo...

nse. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).

Showing 1 - 10 of 24 results

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