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Development Status

US Approved Rx

8

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Primary Target

Inosine-5'-monophosphate dehydrogenase (IMPDH)

6

FK506-binding protein 1A

2

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Highest Phase

Approved

8

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Approval Year

1994

2

1995

6

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Condition

Organ transplant rejection

6

Atopic dermatitis

2

Organ rejection

2

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Treatment Modality

Preventing

8

Primary

2

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CNS Activity

CNS Penetrant

2

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Originator

Gosio, B.

6

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Substance Class

Chemical

8

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Code System

FDA UNII

8

PUBCHEM

8

CAS

7

DAILYMED

6

DRUG BANK

6

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ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

3

DERMATOLOGICALS

2

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ATC Level 2

IMMUNOSUPPRESSANTS

3

OTHER DERMATOLOGICAL PREPARATIONS

2

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ATC Level 3

IMMUNOSUPPRESSANTS

3

OTHER DERMATOLOGICAL PREPARATIONS

2

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ATC Level 4

Calcineurin inhibitors

2

Agents for atopic dermatitis, excluding corticosteroids

1

Agents for dermatitis, excluding corticosteroids

1

Selective immunosuppressants

1

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Substance Form

Salts, Hydrates, Esters, etc.

6

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Showing 1 - 8 of 8 results

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MYCOPHENOLIC ACID

HU9DX48N0T

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

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.

DISODIUM MYCOPHENOLATE

VV8XK6H6MU

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

MYCOPHENOLATE MOFETIL, (Z)-

KI2PVZ8JS6

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

MYCOPHENOLATE MOFETIL

9242ECW6R0

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

MYCOPHENOLATE MOFETIL HYDROCHLORIDE

UXH81S8ZVB

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

MYCOPHENOLATE SODIUM

WX877SQI1G

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Status:

US Approved Rx (2024)

First approved in 1995

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Organ transplant rejection

Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. Mycophenolic acid (MPA) is a fungal metabolite that was initially discovered by Bartolomeo Gosio in 1893 as an antibiotic against ant...

hrax bacillus, Bacillus anthracis. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. It was approved under the brand name Myfortic for the prophylaxis of organ rejection in adult patients receiving a kidney transplant and is indicated for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant. Myfortic is to be used in combination with cyclosporine and corticosteroids.

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.

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