Heart Transplant Rejection

Also known as: Cardiac transplant rejection

DrugDrug NameDrug Description
DB09312Antilymphocyte immunoglobulin (horse)Equine anti-thymocyte globulin is composed of purified gamma globulin containing primarily IgG against human thymus lymphocytes. It is formed by inoculating a horse with an antigen (human thymoyctes) which then induces the horse immune system's B-lymphocytes to produce IgG immunoglobulins specific for that antigen. The result is polyclonal IgG that is then purified from the horse's serum to produce a usable drug product that can be used for immunosuppression. Although the exact mechanism of action is unknown, equine anti-thymocyte globulin targets a variety of immune system proteins including lymphocyte surface proteins, granulocytes, platelets, bone marrow cells, and other cell types. Equine ATG is currently indicated for the suppression of the immune system to prevent renal transplant rejection and in the treatment of aplastic anemia. Induction of T cell apoptosis and resulting T-cell lymphopenia found in vivo is credited for its therapeutic effect in these conditions. There are currently various ATG products available, which differ in the source of inoculated animal (rabbit, horse, or pig) and in the type of antigen product used to produce immunoglobulin (thymocytes, peripheral T cells, etc.).
DB00091CiclosporinCyclosporine is a lipophilic cyclic polypeptide formed by 11 amino acids that presents powerful immunosuppressive and immunomodulatory properties.[A174088] It is isolated from the fungus _Beauveria nivea_ and it was first formulated as an injectable ethanolic solution in 1980 followed by a vegetable oil formulation in 1990.[A174049] This drug was first discovered in 1970 by Sandoz.[A174076] On the FDA records, the first approved product was registered by the company West-Ward Pharmaceuticals International in 1999.[L5149]
DB01590EverolimusEverolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.
DB00688Mycophenolate mofetilMycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (MPA), an immunosuppressive agent, inosine monophosphate dehydrogenase (IMPDH) inhibitor.
DB00877SirolimusA macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
DB00864TacrolimusTacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex inhibits calcineurin which inhibits T-lymphocyte signal transduction and IL-2 transcription.
DrugDrug NameTargetType
DB00091CiclosporinCalcium signal-modulating cyclophilin ligandtarget
DB00091CiclosporinPeptidyl-prolyl cis-trans isomerase Atarget
DB00091CiclosporinCalcineurin subunit B type 2target
DB00091CiclosporinCytochrome P450 3A5enzyme
DB00091CiclosporinCytochrome P450 3A4enzyme
DB00091CiclosporinCytochrome P450 3A7enzyme
DB00091CiclosporinMultidrug resistance protein 1transporter
DB00091CiclosporinCanalicular multispecific organic anion transporter 2transporter
DB00091CiclosporinBile salt export pumptransporter
DB00091CiclosporinSolute carrier organic anion transporter family member 1A2transporter
DB00091CiclosporinIleal sodium/bile acid cotransportertransporter
DB00091CiclosporinSodium/bile acid cotransportertransporter
DB00091CiclosporinSolute carrier family 22 member 6transporter
DB00091CiclosporinMultidrug resistance-associated protein 7transporter
DB00091CiclosporinCanalicular multispecific organic anion transporter 1transporter
DB00091CiclosporinATP-binding cassette sub-family G member 2transporter
DB00091CiclosporinSolute carrier organic anion transporter family member 1B1transporter
DB00091CiclosporinCytochrome P450 2C19enzyme
DB00091CiclosporinCytochrome P450 2C8enzyme
DB00091CiclosporinCytochrome P450 2C9enzyme
DB00091CiclosporinCytochrome P450 2D6enzyme
DB00091CiclosporinPeptidyl-prolyl cis-trans isomerase F, mitochondrialtarget
DB00091CiclosporinSolute carrier organic anion transporter family member 1B3transporter
DB01590EverolimusSerine/threonine-protein kinase mTORtarget
DB01590EverolimusCytochrome P450 3A4enzyme
DB01590EverolimusSolute carrier organic anion transporter family member 1B1transporter
DB01590EverolimusSolute carrier organic anion transporter family member 1B3transporter
DB01590EverolimusSolute carrier organic anion transporter family member 1A2transporter
DB00688Mycophenolate mofetilInosine-5'-monophosphate dehydrogenase 2target
DB00688Mycophenolate mofetilInosine-5'-monophosphate dehydrogenase 1target
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-1enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-7enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-6enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-9enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 2B7enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-8enzyme
DB00688Mycophenolate mofetilUDP-glucuronosyltransferase 1-10enzyme
DB00688Mycophenolate mofetilLiver carboxylesterase 1enzyme
DB00688Mycophenolate mofetilCocaine esteraseenzyme
DB00688Mycophenolate mofetilSerum albumincarrier
DB00688Mycophenolate mofetilCytochrome P450 3A4enzyme
DB00688Mycophenolate mofetilCytochrome P450 3A5enzyme
DB00688Mycophenolate mofetilCytochrome P450 2C8enzyme
DB00688Mycophenolate mofetilSolute carrier organic anion transporter family member 1B1transporter
DB00688Mycophenolate mofetilSolute carrier organic anion transporter family member 1B3transporter
DB00688Mycophenolate mofetilCanalicular multispecific organic anion transporter 1transporter
DB00688Mycophenolate mofetilATP-binding cassette sub-family G member 2transporter
DB00688Mycophenolate mofetilMultidrug resistance protein 1transporter
DB00877SirolimusPeptidyl-prolyl cis-trans isomerase FKBP1Atarget
DB00877SirolimusCytochrome P450 3A4enzyme
DB00877SirolimusSerine/threonine-protein kinase mTORtarget
DB00877SirolimusFibroblast growth factor 2target
DB00877SirolimusCytochrome P450 3A5enzyme
DB00877SirolimusCytochrome P450 3A7enzyme
DB00877SirolimusMultidrug resistance protein 1transporter
DB00877SirolimusSolute carrier organic anion transporter family member 1B1transporter
DB00877SirolimusMultidrug and toxin extrusion protein 1transporter
DB00864TacrolimusPeptidyl-prolyl cis-trans isomerase FKBP1Atarget
DB00864TacrolimusCytochrome P450 3A4enzyme
DB00864TacrolimusCytochrome P450 3A5enzyme
DB00864TacrolimusCytochrome P450 3A7enzyme
DB00864TacrolimusMultidrug resistance protein 1transporter
DB00864TacrolimusATP-binding cassette sub-family A member 5transporter
DB00864TacrolimusSerum albumincarrier
DB00864TacrolimusAlpha-1-acid glycoprotein 1carrier
DB00864TacrolimusSolute carrier organic anion transporter family member 1B1transporter
DrugDrug NamePhaseStatusCount
DB00864Tacrolimus2Recruiting1