- Molecular NameRaltitrexed
- Synonymraltitrexed; ZD-1694; ZD1694
- Weight458.495
- Drugbank_IDDB00293
- ACS_NO112887-68-0
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)0.37
- pka4.5
- LogD (pH=7, predicted)-4.54
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)0.34
- LogSw (predicted, AB/LogsW2.0)0.03
- Sw (mg/ml) (predicted, ACD/Labs)2.22
- No.of HBond Donors4
- No.of HBond Acceptors10
- No.of Rotatable Bonds9
- TPSA176.64
- StatusFDA approved
- AdministrationIntravenous
- PharmacologyA drug in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting Dihydrofolate reductase, an enzyme used in the synthesis of tetrahydrofolate, thereby preventing the synthesis of thymidylate. Raltitrexed is fully active after polyglutamylation. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability15.0
- Protein binding93.0
- Volume of distribution (VD)Steady state, 548 L
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmInside the cell it is extensively polyglutamated by the enzyme folyl polyglutamate synthetase to polyglutamate forms.
- Half life257 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySide effects include pale skin, troubled breathing, unusual bleeding or bruising, unusual tiredness or weakness, black, tarry stools, chest pain, chills, cough, fever, painful or difficult urination, shortness of breath, sore throat, sores, ulcers, or white spots on lips or in mouth, swollen glands, increase in bowel movements, loose stools, soft stools.
- LD50 (rat)N/A
- LD50 (mouse)N/A