Raltitrexed (Tomudex, ZD1694) is a novel quinazoline folate analog that selectively inhibits thymidylate synthase. Raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
| Molecular Weight | 458.49 |
| Formula | C21H22N4O6S |
| CAS Number | 112887-68-0 |
| Solubility (25°C) | DMSO 78 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Bernard Royer, et al. Exposure-response analysis of Raltitrexed assessing liver toxicity
[2] Y Liu, et al. Raltitrexed-based chemotherapy for advanced colorectal cancer
[3] Veerle F Surmont, et al. Raltitrexed in mesothelioma
[4] Kenneth S Wilson, et al. Raltitrexed: optimism and reality
[5] E Van Cutsem, et al. Raltitrexed: current clinical status and future directions
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