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Identification
NameThiotepa
Accession NumberDB04572
TypeSmall Molecule
GroupsApproved
DescriptionN,N'N'-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. It is a stable derivative of N,N',N''- triethylenephosphoramide (TEPA). It is mostly used to treat breast cancer, ovarian cancer and bladder cancer. It is also used as conditioning for Bone marrow transplantation. Its main toxicity is myelosuppression.
Structure
Thumb
Synonyms
Thioplex
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thio Tepa Inj 15mg/vialpowder for solution15 mgoral; rectal; surgical; vaginalLederle Cyanamid Canada Inc.1959-12-311997-11-24Canada
Thiotepa - (pws 15 Mg/vial)powder for solution15 mgintracavitary; intravesicular; intravenousWyeth Canada1997-08-252004-09-15Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thiotepainjection, powder, lyophilized, for solution15 mg/1.5mLintracavitary; intravenous; intravesicalWest Ward Pharmaceuticals Corp2001-06-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII905Z5W3GKH
CAS number52-24-4
WeightAverage: 189.218
Monoisotopic: 189.048954601
Chemical FormulaC6H12N3PS
InChI KeyInChIKey=FOCVUCIESVLUNU-UHFFFAOYSA-N
InChI
InChI=1S/C6H12N3PS/c11-10(7-1-2-7,8-3-4-8)9-5-6-9/h1-6H2
IUPAC Name
tris(aziridin-1-yl)-λ⁵-phosphanethione
SMILES
S=P(N1CC1)(N1CC1)N1CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as organic thiophosphoric acids and derivatives. These are organic compounds containing the thiophosphoric acid functional group or a derivative thereof, with the general structure RP(R')(R'')=S, where R,R',R'' = O,N, halogen residue.
KingdomOrganic compounds
Super ClassOrganophosphorus compounds
ClassOrganothiophosphorus compounds
Sub ClassOrganic thiophosphoric acids and derivatives
Direct ParentOrganic thiophosphoric acids and derivatives
Alternative Parents
Substituents
  • Organic thiophosphoric acid or derivatives
  • Azacycle
  • Organoheterocyclic compound
  • Aziridine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationThioTEPA is used a as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients. Also, when high dose chemotherapy with HPCT support it is appropriate for the treatment of solid tumours in adult and paediatric patients.
PharmacodynamicsThe unstable nitrogen-carbon groups alkylate with DNA causing irrepairable DNA damage. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Mechanism of actionThe alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationUrinary excretion of 14C-labeled thiotepa and metabolites in a 34-year old patient with metastatic carcinoma of the cecum who received a dose of 0.3 mg/kg intravenously was 63%.
Half life1.5 to 4.1 hours
Clearance
  • 446 +/- 63 mL/min [female patients (45 to 84 years) with advanced stage ovarian cancer receiving 60 mg and 80 mg thiotepa by intravenous infusion on subsequent courses given at 4-week intervals]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8788
Blood Brain Barrier+0.9823
Caco-2 permeable-0.5097
P-glycoprotein substrateNon-substrate0.7362
P-glycoprotein inhibitor INon-inhibitor0.8096
P-glycoprotein inhibitor IINon-inhibitor0.9946
Renal organic cation transporterNon-inhibitor0.7874
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7558
CYP450 1A2 substrateNon-inhibitor0.6474
CYP450 2C9 inhibitorNon-inhibitor0.7225
CYP450 2D6 inhibitorNon-inhibitor0.8794
CYP450 2C19 inhibitorNon-inhibitor0.593
CYP450 3A4 inhibitorNon-inhibitor0.8618
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7358
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.8992
BiodegradationNot ready biodegradable0.8949
Rat acute toxicity3.8842 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7707
hERG inhibition (predictor II)Non-inhibitor0.866
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder for solutionoral; rectal; surgical; vaginal15 mg
Injection, powder, lyophilized, for solutionintracavitary; intravenous; intravesical15 mg/1.5mL
Powder for solutionintracavitary; intravesicular; intravenous15 mg
Prices
Unit descriptionCostUnit
Thiotepa 30 mg vial285.0USD vial
Thiotepa 15 mg vial69.6USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point51.5 °CPhysProp
water solubility1.9E+005 mg/L (at 25 °C)MERCK INDEX (1996)
logP0.53HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility9.27 mg/mLALOGPS
logP0.17ALOGPS
logP-1ChemAxon
logS-1.3ALOGPS
pKa (Strongest Basic)-0.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area9.03 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity50.72 m3·mol-1ChemAxon
Polarizability18.23 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-00kn-6900000000-6d6b7c109663ea65ad79View in MoNA
References
Synthesis Reference

John Kazan, “Process for producing thiotepa.” U.S. Patent US4918199, issued February, 1954.

US4918199
General References
  1. Maanen MJ, Smeets CJ, Beijnen JH: Chemistry, pharmacology and pharmacokinetics of N,N',N" -triethylenethiophosphoramide (ThioTEPA). Cancer Treat Rev. 2000 Aug;26(4):257-68. [PubMed:10913381 ]
External Links
ATC CodesL01AC01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Thiotepa.
AmiodaroneThe metabolism of Thiotepa can be decreased when combined with Amiodarone.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Thiotepa.
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Thiotepa.
AprepitantThe serum concentration of Thiotepa can be increased when it is combined with Aprepitant.
ArtemetherThe metabolism of Artemether can be decreased when combined with Thiotepa.
AtazanavirThe metabolism of Thiotepa can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Thiotepa can be decreased when combined with Atomoxetine.
BanoxantroneThe metabolism of Banoxantrone can be decreased when combined with Thiotepa.
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Thiotepa.
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Thiotepa.
BevacizumabBevacizumab may increase the cardiotoxic activities of Thiotepa.
BexaroteneThe serum concentration of Thiotepa can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Thiotepa can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Thiotepa can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Thiotepa can be decreased when it is combined with Bosentan.
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Thiotepa.
BupropionThe serum concentration of Bupropion can be increased when it is combined with Thiotepa.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Thiotepa.
CarbamazepineThe metabolism of Thiotepa can be increased when combined with Carbamazepine.
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Thiotepa.
CeritinibThe serum concentration of Thiotepa can be increased when it is combined with Ceritinib.
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Thiotepa.
CisaprideThe metabolism of Cisapride can be decreased when combined with Thiotepa.
ClarithromycinThe metabolism of Thiotepa can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Thiotepa can be decreased when combined with Clemastine.
ClobazamThe metabolism of Clobazam can be decreased when combined with Thiotepa.
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Thiotepa.
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Thiotepa.
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Thiotepa.
ClotrimazoleThe metabolism of Thiotepa can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Thiotepa is combined with Clozapine.
CobicistatThe metabolism of Thiotepa can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Thiotepa can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Thiotepa can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Thiotepa.
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Thiotepa.
CyclosporineThe metabolism of Thiotepa can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Thiotepa can be decreased when it is combined with Dabrafenib.
DarunavirThe metabolism of Thiotepa can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Thiotepa can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Thiotepa can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Thiotepa can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Thiotepa.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Thiotepa.
DexamethasoneThe serum concentration of Thiotepa can be decreased when it is combined with Dexamethasone.
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Thiotepa.
DiazepamThe metabolism of Diazepam can be decreased when combined with Thiotepa.
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Thiotepa.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Thiotepa.
DigoxinDigoxin may decrease the cardiotoxic activities of Thiotepa.
DihydroergotamineThe metabolism of Thiotepa can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Thiotepa can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Thiotepa.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Thiotepa.
DomperidoneThe metabolism of Domperidone can be decreased when combined with Thiotepa.
DoxycyclineThe metabolism of Thiotepa can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Thiotepa can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Thiotepa can be decreased when it is combined with Efavirenz.
EfavirenzThe metabolism of Efavirenz can be decreased when combined with Thiotepa.
EnzalutamideThe serum concentration of Thiotepa can be decreased when it is combined with Enzalutamide.
EpinastineThe metabolism of Epinastine can be decreased when combined with Thiotepa.
ErythromycinThe metabolism of Thiotepa can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Thiotepa can be decreased when it is combined with Eslicarbazepine acetate.
EstroneThe metabolism of Estrone can be decreased when combined with Thiotepa.
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Thiotepa.
EtravirineThe serum concentration of Thiotepa can be decreased when it is combined with Etravirine.
FingolimodThiotepa may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe metabolism of Thiotepa can be decreased when combined with Fluconazole.
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Thiotepa.
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Thiotepa.
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Thiotepa.
FluvoxamineThe metabolism of Thiotepa can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Thiotepa can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Thiotepa can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Thiotepa can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Thiotepa can be increased when it is combined with Fusidic Acid.
HalothaneThe metabolism of Halothane can be decreased when combined with Thiotepa.
IdelalisibThe serum concentration of Thiotepa can be increased when it is combined with Idelalisib.
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Thiotepa.
ImatinibThe metabolism of Thiotepa can be decreased when combined with Imatinib.
ImipramineThe metabolism of Imipramine can be decreased when combined with Thiotepa.
IndinavirThe metabolism of Thiotepa can be decreased when combined with Indinavir.
IrinotecanThe metabolism of Irinotecan can be decreased when combined with Thiotepa.
IsavuconazoniumThe metabolism of Thiotepa can be decreased when combined with Isavuconazonium.
IsofluraneThe metabolism of Isoflurane can be decreased when combined with Thiotepa.
IsradipineThe metabolism of Thiotepa can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Thiotepa can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Thiotepa can be increased when it is combined with Ivacaftor.
IxazomibThe metabolism of Ixazomib can be decreased when combined with Thiotepa.
KetamineThe metabolism of Ketamine can be decreased when combined with Thiotepa.
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Thiotepa.
KetoconazoleThe metabolism of Thiotepa can be decreased when combined with Ketoconazole.
LeflunomideThe risk or severity of adverse effects can be increased when Thiotepa is combined with Leflunomide.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Thiotepa.
LoperamideThe metabolism of Loperamide can be decreased when combined with Thiotepa.
LopinavirThe metabolism of Thiotepa can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Thiotepa.
LovastatinThe metabolism of Thiotepa can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Thiotepa can be increased when it is combined with Luliconazole.
MalathionThe metabolism of Malathion can be decreased when combined with Thiotepa.
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Thiotepa.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Thiotepa.
MethadoneThe metabolism of Methadone can be decreased when combined with Thiotepa.
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Thiotepa.
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Thiotepa.
MethyltestosteroneThe metabolism of Methyltestosterone can be decreased when combined with Thiotepa.
MexiletineThe metabolism of Mexiletine can be decreased when combined with Thiotepa.
MianserinThe metabolism of Mianserin can be decreased when combined with Thiotepa.
MidazolamThe metabolism of Midazolam can be decreased when combined with Thiotepa.
MifepristoneThe metabolism of Thiotepa can be decreased when combined with Mifepristone.
MitotaneThe serum concentration of Thiotepa can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Thiotepa can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Thiotepa can be decreased when it is combined with Nafcillin.
NatalizumabThe risk or severity of adverse effects can be increased when Thiotepa is combined with Natalizumab.
NefazodoneThe metabolism of Thiotepa can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Thiotepa can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Thiotepa can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Thiotepa can be decreased when combined with Nevirapine.
NicotineThe metabolism of Nicotine can be decreased when combined with Thiotepa.
NilotinibThe metabolism of Thiotepa can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Thiotepa can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Thiotepa can be increased when it is combined with Osimertinib.
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Thiotepa.
OuabainOuabain may decrease the cardiotoxic activities of Thiotepa.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Thiotepa.
PalbociclibThe serum concentration of Thiotepa can be increased when it is combined with Palbociclib.
PentobarbitalThe metabolism of Thiotepa can be increased when combined with Pentobarbital.
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Thiotepa.
PermethrinThe metabolism of Permethrin can be decreased when combined with Thiotepa.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Thiotepa.
PethidineThe metabolism of Pethidine can be decreased when combined with Thiotepa.
PhenobarbitalThe metabolism of Thiotepa can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Thiotepa can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Thiotepa.
PosaconazoleThe metabolism of Thiotepa can be decreased when combined with Posaconazole.
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Thiotepa.
PrimidoneThe metabolism of Thiotepa can be increased when combined with Primidone.
PromethazineThe metabolism of Promethazine can be decreased when combined with Thiotepa.
PropofolThe metabolism of Propofol can be decreased when combined with Thiotepa.
Rabies vaccineThe risk or severity of adverse effects can be increased when Thiotepa is combined with Rabies vaccine.
RanolazineThe metabolism of Thiotepa can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Thiotepa can be increased when combined with Rifabutin.
RifampicinThe metabolism of Thiotepa can be increased when combined with Rifampicin.
RifapentineThe metabolism of Thiotepa can be increased when combined with Rifapentine.
RitonavirThe metabolism of Thiotepa can be decreased when combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Thiotepa.
RomidepsinThe metabolism of Romidepsin can be decreased when combined with Thiotepa.
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Thiotepa.
SaquinavirThe metabolism of Thiotepa can be decreased when combined with Saquinavir.
SelegilineThe metabolism of Selegiline can be decreased when combined with Thiotepa.
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Thiotepa.
SertralineThe metabolism of Sertraline can be decreased when combined with Thiotepa.
SevofluraneThe metabolism of Sevoflurane can be decreased when combined with Thiotepa.
SildenafilThe metabolism of Thiotepa can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Thiotepa can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Thiotepa can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Thiotepa.
SorafenibThe metabolism of Sorafenib can be decreased when combined with Thiotepa.
St. John's WortThe serum concentration of Thiotepa can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Thiotepa can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Thiotepa can be decreased when combined with Sulfisoxazole.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thiotepa.
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Thiotepa.
TelaprevirThe metabolism of Thiotepa can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Thiotepa can be decreased when combined with Telithromycin.
TemazepamThe metabolism of Temazepam can be decreased when combined with Thiotepa.
TestosteroneThe metabolism of Testosterone can be decreased when combined with Thiotepa.
TiclopidineThe metabolism of Thiotepa can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Thiotepa can be decreased when it is combined with Tocilizumab.
TofacitinibThiotepa may increase the immunosuppressive activities of Tofacitinib.
TramadolThe metabolism of Tramadol can be decreased when combined with Thiotepa.
TrastuzumabTrastuzumab may increase the neutropenic activities of Thiotepa.
TretinoinThe metabolism of Tretinoin can be decreased when combined with Thiotepa.
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Thiotepa.
VenlafaxineThe metabolism of Thiotepa can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Thiotepa can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Thiotepa can be decreased when combined with Voriconazole.
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Thiotepa.
ZiprasidoneThe metabolism of Thiotepa can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
cross-linking/alkylation
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Gor PP, Su HI, Gray RJ, Gimotty PA, Horn M, Aplenc R, Vaughan WP, Tallman MS, Rebbeck TR, DeMichele A: Cyclophosphamide-metabolizing enzyme polymorphisms and survival outcomes after adjuvant chemotherapy for node-positive breast cancer: a retrospective cohort study. Breast Cancer Res. 2010;12(3):R26. doi: 10.1186/bcr2570. Epub 2010 May 10. [PubMed:20459744 ]
  2. Lee PC, Kakadiya R, Su TL, Lee TC: Combination of bifunctional alkylating agent and arsenic trioxide synergistically suppresses the growth of drug-resistant tumor cells. Neoplasia. 2010 May;12(5):376-87. [PubMed:20454509 ]
  3. Lestuzzi C: Neoplastic pericardial disease: Old and current strategies for diagnosis and management. World J Cardiol. 2010 Sep 26;2(9):270-9. doi: 10.4330/wjc.v2.i9.270. [PubMed:21160603 ]
  4. Maanen MJ, Smeets CJ, Beijnen JH: Chemistry, pharmacology and pharmacokinetics of N,N',N" -triethylenethiophosphoramide (ThioTEPA). Cancer Treat Rev. 2000 Aug;26(4):257-68. [PubMed:10913381 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on September 07, 2007 14:54 / Updated on August 17, 2016 12:24