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SIROLIMUS Drug Record

  • Summary
  • Interactions
  • Claims
  • SIROLIMUS chembl:CHEMBL413 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    RAPAMYCIN
    SIROLIMUS
    L04AA10
    RAPAMUNE
    SM-88 COMPONENT SIROLIMUS
    AY-22989
    WY-090217
    NSC-226080
    (-)-RAPAMYCIN
    drugbank:00877
    chembl:CHEMBL413
    pubchem.compound:5284616
    rxcui:35302
    chemidplus:53123-88-9

    Drug Info:

    Notes rapalogue
    Drug Class Kinase Inhibitors
    Drug Indications for treatment of wet age-related macular degeneration
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications immunosuppressant
    Drug Class immunosuppressive agents
    Year of Approval 2007
    (14 More Sources)

    Publications:

    Nardacci et al., 2005, Characterization of cell death pathways in human immunodeficiency virus-associated encephalitis., Am. J. Pathol.
    Yamaguchi et al., 2016, A synthetic-lethality RNAi screen reveals an ERK-mTOR co-targeting pro-apoptotic switch in PIK3CA+ oral cancers., Oncotarget
    Purdom-Dickinson et al., 2007, Translational control of nrf2 protein in activation of antioxidant response by oxidants., Mol. Pharmacol.
    Jardim et al., 2014, FBXW7 mutations in patients with advanced cancers: clinical and molecular characteristics and outcomes with mTOR inhibitors., PLoS ONE
    Mao et al., 2008, FBXW7 targets mTOR for degradation and cooperates with PTEN in tumor suppression., Science
    Wang et al., 2013, Rapamycin inhibits FBXW7 loss-induced epithelial-mesenchymal transition and cancer stem cell-like characteristics in colorectal cancer cells., Biochem. Biophys. Res. Commun.
    Nepomuceno et al., 2003, Rapamycin inhibits the interleukin 10 signal transduction pathway and the growth of Epstein Barr virus B-cell lymphomas., Cancer Res.
    Sam WJ et al., 2011, Associations of ABCB1 3435C>T and IL-10-1082G>A polymorphisms with long-term sirolimus dose requirements in renal transplant patients., Transplantation
    Woillard JB et al., 2013, Effect of CYP3A4*22, POR*28, and PPARA rs4253728 on sirolimus in vitro metabolism and trough concentrations in kidney transplant recipients., Clin Chem
    Liang et al., 2010, TSC1 loss synergizes with KRAS activation in lung cancer development in the mouse and confers rapamycin sensitivity., Oncogene
    Avellino et al., 2005, Rapamycin stimulates apoptosis of childhood acute lymphoblastic leukemia cells., Blood
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Engelman et al., 2008, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers., Nat. Med.
    Kang et al., 2005, Phosphatidylinositol 3-kinase mutations identified in human cancer are oncogenic., Proc. Natl. Acad. Sci. U.S.A.
    Gymnopoulos et al., 2007, Rare cancer-specific mutations in PIK3CA show gain of function., Proc. Natl. Acad. Sci. U.S.A.
    Mavrakis et al., 2008, Tumorigenic activity and therapeutic inhibition of Rheb GTPase., Genes Dev.
    Sehgal, 2003, Sirolimus: its discovery, biological properties, and mechanism of action., Transplant. Proc.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Salomé C et al., 2014, Benzofuran derivatives as anticancer inhibitors of mTOR signaling., Eur J Med Chem
    Du L et al., 2014, Cytotoxic dimeric epipolythiodiketopiperazines from the ascomycetous fungus Preussia typharum., J Nat Prod
    Nowak P et al., 2009, Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase., J Med Chem
    Pratt MR et al., 2007, Small-molecule-mediated rescue of protein function by an inducible proteolytic shunt., Proc Natl Acad Sci U S A
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Grabiner et al., 2014, A diverse array of cancer-associated MTOR mutations are hyperactivating and can predict rapamycin sensitivity., Cancer Discov
    Rodrik-Outmezguine et al., 2016, Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor., Nature
    Shuuin et al., 2009, [Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma]., Gan To Kagaku Ryoho
    Dowling et al., 2010, Dissecting the role of mTOR: lessons from mTOR inhibitors., Biochim. Biophys. Acta
    Xu et al., 2016, Mechanistically distinct cancer-associated mTOR activation clusters predict sensitivity to rapamycin., J. Clin. Invest.
    Lovly et al., 2011, Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors., Cancer Res.
    Mungamuri et al., 2006, Survival signaling by Notch1: mammalian target of rapamycin (mTOR)-dependent inhibition of p53., Cancer Res.
    Palm et al., 2015, The Utilization of Extracellular Proteins as Nutrients Is Suppressed by mTORC1., Cell
    Contreras et al., Lkb1 inactivation is sufficient to drive endometrial cancers that are aggressive yet highly responsive to mTOR inhibitor monotherapy., Dis Model Mech
    Brown et al., 2003, Rapamycin is active against B-precursor leukemia in vitro and in vivo, an effect that is modulated by IL-7-mediated signaling., Proc. Natl. Acad. Sci. U.S.A.
    Ganesan et al., 2016, Epidermal Growth Factor Receptor P753S Mutation in Cutaneous Squamous Cell Carcinoma Responsive to Cetuximab-Based Therapy., J. Clin. Oncol.
    Pirazzoli et al., 2014, Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1., Cell Rep
    Engelman et al., 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib., Cancer Res.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Mbatchi LC et al., 2017, Association of NR1I2, CYP3A5 and ABCB1 genetic polymorphisms with variability of temsirolimus pharmacokinetics and toxicity in patients with metastatic bladder cancer., Cancer Chemother Pharmacol
    Woillard JB et al., 2010, Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant allele., Br J Clin Pharmacol
    Aoki et al., 2006, mTOR pathway inhibition attenuates skeletal muscle growth induced by stretching., Cell Tissue Res.
    Maertens et al., 2013, Elucidating distinct roles for NF1 in melanomagenesis., Cancer Discov
    Pawarode et al., 2007, Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins., Cancer Chemother. Pharmacol.
    Wei et al., 2006, Gene expression-based chemical genomics identifies rapamycin as a modulator of MCL1 and glucocorticoid resistance., Cancer Cell
    Dunn et al., 2001, Up-regulation of urokinase-type plasminogen activator by insulin-like growth factor-I depends upon phosphatidylinositol-3 kinase and mitogen-activated protein kinase kinase., Cancer Res.
    Chen et al., 1996, The RB/p107/p130 phosphorylation pathway is not inhibited in rapamycin-induced G1-prolongation of NIH3T3 cells., Oncogene
    Entingh et al., 2001, Induction of the C/EBP homologous protein (CHOP) by amino acid deprivation requires insulin-like growth factor I, phosphatidylinositol 3-kinase, and mammalian target of rapamycin signaling., Endocrinology
    Tirado et al., 2005, Rapamycin induces apoptosis of JN-DSRCT-1 cells by increasing the Bax : Bcl-xL ratio through concurrent mechanisms dependent and independent of its mTOR inhibitory activity., Oncogene
    Cummins et al., 2004, CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam., J. Pharmacol. Exp. Ther.
    Sam WJ et al., 2012, Associations of ABCB1 and IL-10 genetic polymorphisms with sirolimus-induced dyslipidemia in renal transplant recipients., Transplantation
    Lai et al., 1994, CD28 signaling causes a sustained down-regulation of I kappa B alpha which can be prevented by the immunosuppressant rapamycin., J. Biol. Chem.
    Vanasek et al., 2001, Antagonistic roles for CTLA-4 and the mammalian target of rapamycin in the regulation of clonal anergy: enhanced cell cycle progression promotes recall antigen responsiveness., J. Immunol.
    Fox et al., 2005, The Pim kinases control rapamycin-resistant T cell survival and activation., J. Exp. Med.
    Renoir et al., 1992, [Effect of immunosuppressants FK506 and rapamycin on the function of progesterone receptor: protein "p59-HBI", intersection between immunology and endocrinology?]., C. R. Acad. Sci. III, Sci. Vie
    Patel et al., 2002, Insulin regulation of hepatic insulin-like growth factor-binding protein-1 (IGFBP-1) gene expression and mammalian target of rapamycin (mTOR) signalling is impaired by the presence of hydrogen peroxide., Biochem. J.
    Livi et al., 2013, Rapamycin extends life span of Rb1+/- mice by inhibiting neuroendocrine tumors., Aging (Albany NY)
    Windle et al., 1990, Retinoblastoma in transgenic mice., Nature
    Piña et al., 2011, Advanced retinoblastoma treatment: targeting hypoxia by inhibition of the mammalian target of rapamycin (mTOR) in LH(BETA)T(AG) retinal tumors., Clin Ophthalmol
    Bierer et al., 1990, Probing immunosuppressant action with a nonnatural immunophilin ligand., Science
    Fraser et al., 1999, The association of initiation factor 4F with poly(A)-binding protein is enhanced in serum-stimulated Xenopus kidney cells., J. Biol. Chem.
    Feigenblum et al., 1996, Cap-binding protein (eukaryotic initiation factor 4E) and 4E-inactivating protein BP-1 independently regulate cap-dependent translation., Mol. Cell. Biol.
    Naegele et al., 2004, Molecular cross-talk between MEK1/2 and mTOR signaling during recovery of 293 cells from hypertonic stress., J. Biol. Chem.
    Davies et al., 2004, Inhibition of phosphatidylinositol 3-kinase- and ERK MAPK-regulated protein synthesis reveals the pro-apoptotic properties of CD40 ligation in carcinoma cells., J. Biol. Chem.
    Tuxworth et al., 1999, Role of load in regulating eIF-4F complex formation in adult feline cardiocytes., Am. J. Physiol.
    Fraser et al., 1999, Cellular stress in xenopus kidney cells enhances the phosphorylation of eukaryotic translation initiation factor (eIF)4E and the association of eIF4F with poly(A)-binding protein., Biochem. J.
    Sanftner et al., 2006, Dimerizer regulation of AADC expression and behavioral response in AAV-transduced 6-OHDA lesioned rats., Mol. Ther.
    Duncan et al., 2005, Signal transduction pathways leading to increased eIF4E phosphorylation caused by oxidative stress., Free Radic. Biol. Med.
    Hahn-Windgassen et al., 2005, Akt activates the mammalian target of rapamycin by regulating cellular ATP level and AMPK activity., J. Biol. Chem.
    Hung et al., 2010, Development of a mouse model for sporadic and metastatic colon tumors and its use in assessing drug treatment., Proc. Natl. Acad. Sci. U.S.A.
    Fujishita et al., 2008, Inhibition of the mTORC1 pathway suppresses intestinal polyp formation and reduces mortality in ApcDelta716 mice., Proc. Natl. Acad. Sci. U.S.A.
    Vanaudenaerde et al., 2007, Macrolides inhibit IL17-induced IL8 and 8-isoprostane release from human airway smooth muscle cells., Am. J. Transplant.
    Rodríguez-Jiménez C et al., 2017, Influence of genetic polymorphisms of CYP3A5 and ABCB1 on sirolimus pharmacokinetics, patient and graft survival and other clinical outcomes in renal transplant., Drug Metab Pers Ther
    Li Y et al., 2015, CYP3A5 and ABCB1 genotype influence tacrolimus and sirolimus pharmacokinetics in renal transplant recipients., Springerplus
    Emoto C et al., 2015, The impact of CYP3A5*3 polymorphism on sirolimus pharmacokinetics: insights from predictions with a physiologically-based pharmacokinetic model., Br J Clin Pharmacol
    Miao LY et al., 2008, Association study of ABCB1 and CYP3A5 gene polymorphisms with sirolimus trough concentration and dose requirements in Chinese renal transplant recipients., Biopharm Drug Dispos
    Le Meur Y et al., 2006, CYP3A5*3 influences sirolimus oral clearance in de novo and stable renal transplant recipients., Clin Pharmacol Ther
    Anglicheau D et al., 2005, Consequences of genetic polymorphisms for sirolimus requirements after renal transplant in patients on primary sirolimus therapy., Am J Transplant
    Singleton et al., 2015, Kinome RNAi Screens Reveal Synergistic Targeting of MTOR and FGFR1 Pathways for Treatment of Lung Cancer and HNSCC., Cancer Res.
    Dubois et al., 2003, Distinct pathways involving the FK506-binding proteins 12 and 12.6 underlie IL-2-versus IL-15-mediated proliferation of T cells., Proc. Natl. Acad. Sci. U.S.A.
    Schalm et al., 2002, Identification of a conserved motif required for mTOR signaling., Curr. Biol.
    Martin et al., 2001, Ribosomal S6 kinase 2 inhibition by a potent C-terminal repressor domain is relieved by mitogen-activated protein-extracellular signal-regulated kinase kinase-regulated phosphorylation., J. Biol. Chem.
    Martin et al., 2001, Regulation of ribosomal S6 kinase 2 by effectors of the phosphoinositide 3-kinase pathway., J. Biol. Chem.
    Perera et al., 2009, HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy., Proc. Natl. Acad. Sci. U.S.A.
    Schaefer et al., 2007, Decorin-mediated regulation of fibrillin-1 in the kidney involves the insulin-like growth factor-I receptor and Mammalian target of rapamycin., Am. J. Pathol.
    Poulalhon et al., 2006, Modulation of collagen and MMP-1 gene expression in fibroblasts by the immunosuppressive drug rapamycin. A direct role as an antifibrotic agent?, J. Biol. Chem.
    Poston et al., 1999, Antisense oligodeoxynucleotides prevent acute cardiac allograft rejection via a novel, nontoxic, highly efficient transfection method., Transplantation
    Ling Q et al., 2013, Association between donor and recipient TCF7L2 gene polymorphisms and the risk of new-onset diabetes mellitus after liver transplantation in a Han Chinese population., J Hepatol
    Kurzawski M et al., 2011, Association of transcription factor 7-like 2 (TCF7L2) gene polymorphism with posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus., Pharmacol Rep
    Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood
    Ghosh AP et al., 2015, Point mutations of the mTOR-RHEB pathway in renal cell carcinoma., Oncotarget
    Wu M et al., 2015, Flcn-deficient renal cells are tumorigenic and sensitive to mTOR suppression., Oncotarget
  • SIROLIMUS   EIF4E

    Interaction Score: 2.58

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9867830 8816458 15292274 14581487 10516161 10477262


    Sources:
    NCI

  • SIROLIMUS   DCN

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17200203


    Sources:
    NCI

  • SIROLIMUS   FKBP4

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1700475


    Sources:
    NCI

  • SIROLIMUS   RBL2

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8895523


    Sources:
    NCI

  • SIROLIMUS   IL7

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14657335


    Sources:
    NCI

  • SIROLIMUS   FLCN

    Interaction Score: 1.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26418749


    Sources:
    CIViC

  • SIROLIMUS   RHEB

    Interaction Score: 1.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26255626


    Sources:
    CIViC

  • SIROLIMUS   FKBP1A

    Interaction Score: 0.76

    Interaction Types & Directionality:
    other/unknown
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction FK506-binding protein 1A inhibitor
    Trial Name LCP-Siro, sirolimus

    PMIDs:
    12742462 11752352 24836070 24893224


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND TTD

  • SIROLIMUS   TSC1

    Interaction Score: 0.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19966866


    Sources:
    CIViC

  • SIROLIMUS   FBXW7

    Interaction Score: 0.69

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colon cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    24586741 18787170 23558291


    Sources:
    JAX-CKB CIViC

  • SIROLIMUS   TCF7L2

    Interaction Score: 0.66

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23041303 21857094


    Sources:
    PharmGKB

  • SIROLIMUS   DDC

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16126007


    Sources:
    NCI

  • SIROLIMUS   IL15

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14605212


    Sources:
    NCI

  • SIROLIMUS   WT1

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15782132


    Sources:
    NCI

  • SIROLIMUS   NF1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23171796


    Sources:
    CIViC

  • SIROLIMUS   POR

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23974086


    Sources:
    PharmGKB

  • SIROLIMUS   IL10

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12907620 22094953


    Sources:
    NCI PharmGKB

  • SIROLIMUS   IGFBP1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11942857


    Sources:
    NCI

  • SIROLIMUS   EML4

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sirolimus + X-396
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    21613408


    Sources:
    JAX-CKB

  • SIROLIMUS   RB1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type retinoblastoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    23454836 1689463 21468343


    Sources:
    JAX-CKB

  • SIROLIMUS   UGT1A8

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20565459


    Sources:
    PharmGKB

  • SIROLIMUS   CTLA4

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7982907 11698435


    Sources:
    NCI

  • SIROLIMUS   APC

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colon cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    20080688 18768809


    Sources:
    JAX-CKB

  • SIROLIMUS   MTOR

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name LCP-Siro, sirolimus
    Novel drug target Established target
    Trial Name sirolimus, rapamycin,Perceiva

    PMIDs:
    19848404 24836070 17563385 24893224 26619011 24631838 27279227 19620795 12742462 11752352 20005306 27482884


    Sources:
    TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial DoCM CIViC TTD

  • SIROLIMUS   RPS6KB1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11967149 11108720 11108711


    Sources:
    NCI

  • SIROLIMUS   IL17A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17061983


    Sources:
    NCI

  • SIROLIMUS   ITGAL

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10515383


    Sources:
    NCI

  • SIROLIMUS   MMP1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16914544


    Sources:
    NCI

  • SIROLIMUS   FGF2

    Interaction Score: 0.11

    Interaction Types & Directionality:
    other/unknown

    Interaction Info:
    Trial Name LCP-Siro, sirolimus
    Novel drug target Established target

    PMIDs:
    12742462


    Sources:
    TdgClinicalTrial

  • SIROLIMUS   TGM2

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16127150


    Sources:
    NCI

  • SIROLIMUS   CYP3A5

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28245187 26543771 26256674 23974086 22094953 17941052 16815317 15707415


    Sources:
    PharmGKB

  • SIROLIMUS   STK11

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    20142330


    Sources:
    JAX-CKB

  • SIROLIMUS   PRKAA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16027121


    Sources:
    NCI

  • SIROLIMUS   DDIT3

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11145585


    Sources:
    NCI

  • SIROLIMUS   PLAU

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11245436


    Sources:
    NCI

  • SIROLIMUS   MAPK10

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15683719


    Sources:
    NCI

  • SIROLIMUS   PIM1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15642745


    Sources:
    NCI

  • SIROLIMUS   PIK3CA

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    15878982 28514312 26882569 19029981 15647370 17376864


    Sources:
    JAX-CKB NCI CIViC

  • SIROLIMUS   HRAS

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Sirolimus + Trametinib
    Indication/Tumor Type head and neck squamous cell carcinoma
    Response Type sensitive

    PMIDs:
    26882569


    Sources:
    JAX-CKB

  • SIROLIMUS   NOS1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16408196


    Sources:
    NCI

  • SIROLIMUS   MCL1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17010674


    Sources:
    NCI

  • SIROLIMUS   BAX

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15782132


    Sources:
    NCI

  • SIROLIMUS   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Afatinib + Cetuximab + Sirolimus
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    24934779 24813888 18089823 25157968


    Sources:
    JAX-CKB DoCM CIViC

  • SIROLIMUS   PGR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1284044


    Sources:
    NCI

  • SIROLIMUS   JAK2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22955920


    Sources:
    CIViC

  • SIROLIMUS   ABCG2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17031644


    Sources:
    NCI

  • SIROLIMUS   AKT1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type predicted – sensitive
    combination therapy Doxorubicin + Sirolimus
    Evidence Type Actionable

    PMIDs:
    18708578


    Sources:
    JAX-CKB

  • SIROLIMUS   FGFR1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD4547 + Sirolimus
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    26359452


    Sources:
    JAX-CKB

  • SIROLIMUS   KRAS

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type conflicting
    Approval Status Preclinical

    PMIDs:
    26882569 26144316


    Sources:
    JAX-CKB

  • SIROLIMUS   ABCB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14569063 28676933 23073467


    Sources:
    NCI PharmGKB

  • SIROLIMUS   NR1I2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28676933


    Sources:
    PharmGKB

  • SIROLIMUS   OPRK1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • SIROLIMUS   ERBB2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19122144


    Sources:
    CIViC

  • SIROLIMUS   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type conflicting
    Approval Status Preclinical

    PMIDs:
    16651424 26144316


    Sources:
    JAX-CKB NCI

  • SIROLIMUS   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17652445


    Sources:
    NCI

  • SIROLIMUS   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MyCancerGenome: SIROLIMUS

    • Version: 20-Jun-2017

    Alternate Names:
    AY22989 Development Name
    SILA9268A Development Name
    WY-090217 Development Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes rapalogue

    Publications:

  • TEND: SIROLIMUS

    • Version: 01-August-2011

    Alternate Names:
    SIROLIMUS Primary Drug Name

    Drug Info:
    Year of Approval 2007
    Drug Class immunosuppressive agents

    Publications:

  • TdgClinicalTrial: SIROLIMUS

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications immunosuppressant
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • DTC: SIROLIMUS

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL413 ChEMBL Drug ID

    Drug Info:

    Publications:
    Nowak P et al., 2009, Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase., J Med Chem
    Pratt MR et al., 2007, Small-molecule-mediated rescue of protein function by an inducible proteolytic shunt., Proc Natl Acad Sci U S A
    Du L et al., 2014, Cytotoxic dimeric epipolythiodiketopiperazines from the ascomycetous fungus Preussia typharum., J Nat Prod

  • NCI: RAPAMYCIN

    • Version: 14-September-2017

    Alternate Names:
    C1212 NCI drug code

    Drug Info:

    Publications:
    Nardacci et al., 2005, Characterization of cell death pathways in human immunodeficiency virus-associated encephalitis., Am. J. Pathol.
    Purdom-Dickinson et al., 2007, Translational control of nrf2 protein in activation of antioxidant response by oxidants., Mol. Pharmacol.
    Wei et al., 2006, Gene expression-based chemical genomics identifies rapamycin as a modulator of MCL1 and glucocorticoid resistance., Cancer Cell

  • NCI: SIROLIMUS

    • Version: 14-September-2017

    Alternate Names:
    C1212 NCI drug code

    Drug Info:

    Publications:
    Pawarode et al., 2007, Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins., Cancer Chemother. Pharmacol.
    Cummins et al., 2004, CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam., J. Pharmacol. Exp. Ther.

  • PharmGKB: sirolimus

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Woillard JB et al., 2013, Effect of CYP3A4*22, POR*28, and PPARA rs4253728 on sirolimus in vitro metabolism and trough concentrations in kidney transplant recipients., Clin Chem
    Woillard JB et al., 2010, Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant allele., Br J Clin Pharmacol
    Mbatchi LC et al., 2017, Association of NR1I2, CYP3A5 and ABCB1 genetic polymorphisms with variability of temsirolimus pharmacokinetics and toxicity in patients with metastatic bladder cancer., Cancer Chemother Pharmacol

  • JAX-CKB: Sirolimus

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Jardim et al., 2014, FBXW7 mutations in patients with advanced cancers: clinical and molecular characteristics and outcomes with mTOR inhibitors., PLoS ONE
    Mao et al., 2008, FBXW7 targets mTOR for degradation and cooperates with PTEN in tumor suppression., Science
    Wang et al., 2013, Rapamycin inhibits FBXW7 loss-induced epithelial-mesenchymal transition and cancer stem cell-like characteristics in colorectal cancer cells., Biochem. Biophys. Res. Commun.

  • DoCM: RAPAMYCIN

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Grabiner et al., 2014, A diverse array of cancer-associated MTOR mutations are hyperactivating and can predict rapamycin sensitivity., Cancer Discov

  • DoCM: SIROLIMUS

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Ganesan et al., 2016, Epidermal Growth Factor Receptor P753S Mutation in Cutaneous Squamous Cell Carcinoma Responsive to Cetuximab-Based Therapy., J. Clin. Oncol.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Engelman et al., 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib., Cancer Res.

  • CIViC: SIROLIMUS

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Perera et al., 2009, HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy., Proc. Natl. Acad. Sci. U.S.A.
    Ganesan et al., 2016, Epidermal Growth Factor Receptor P753S Mutation in Cutaneous Squamous Cell Carcinoma Responsive to Cetuximab-Based Therapy., J. Clin. Oncol.
    Maertens et al., 2013, Elucidating distinct roles for NF1 in melanomagenesis., Cancer Discov

  • TALC: SIROLIMUS

    • Version: 12-May-2016

    Alternate Names:
    SIROLIMUS Primary Drug Name
    SIROLIMUS Drug Generic Name
    RAPAMUNE Drug Trade Name

    Drug Info:

    Publications:

  • TTD: Sirolimus

    • Version: 2020.06.01

    Alternate Names:
    D03LJR TTD Drug ID

    Drug Info:

    Publications:

  • TTD: Rapamycin

    • Version: 2020.06.01

    Alternate Names:
    D0T6DK TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL413

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL413

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: RAPAMYCIN

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: SIROLIMUS

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21