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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
TEMSIROLIMUS (has an active metabolite)

TEMSIROLIMUS


ATC L01EG01

ANTINEOPLASTIC AGENTS
TREATMENT OF ADVANCED RENAL CELL CARCINOMA
PROTEIN-PROTEIN INTERACTION INHIBITOR FKBP12 / MTOR (MAMMALIAN TARGET OF RAPAMYCIN)
TREATMENT OF MANTLE CELL LYMPHOMA (MCL) (DRUG FOR RARE DISEASE IN EUROPE)

INTRAVENOUS

Cmax 056 MICROMOLAR (25 MILLIGRAM)

VD 172 LITER

Cl 16.2 LITER / HOUR

HT 17.3 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER

FK506 BINDING PROTEIN-12 (FKBP-12)/MTOR COMPLEX

PDB 7SQ9 (CRYO-EM STRUCTURE OF MOUSE TEMSIROLIMUS, PI(3,5)P2-BOUND TRPML1 CHANNEL AT 2.11 ANGSTROM RESOLUTION)

LIGAND CODE = A4I (link to the list of PDB complexes)

Download experimental 3D coordinates of A4I with added hydrogens

Peptidyl-prolyl cis-trans isomerase FKBP1A UNIPROT P62942 FKBP1A

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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