Table 1.
Antitumor marine natural compounds in clinical trials with preclinical toxicity evaluation in animals.
| Compound | Phase of clinical trails | Animal model | Toxicities |
|---|---|---|---|
| Bryostatin-1 | II | Mice | In mice, toxicities include lethargy, unsteadiness, |
| haematuria, and myelosuppression [8]. | |||
| Dolastatin-10 | II | Mice, rats, dogs | Maximum tolerated doses of 1350 μg/m2 (mice), |
| 450 μg/m2 (rats), and ∼ 400 μg/m2 (dogs); Myelotoxicity | |||
| was the most severe dose-limiting effect [9]. | |||
| LU103793a | II | N/A | Toxic effects in hematopoietic, lymphoid |
| systems, gastrointestinal tract, and heart [8]. | |||
| Discodermolidea | I | Mice | Immunosuppresive [10]. |
| Yondelis | II/III | Mice, rats, monkeys | Reversible hepatobiliary toxicity in monkeys [11]. |
| Hematotoxic at MTD 600 μg/m2 in mice [12]. | |||
| Hepatotoxic in rats [13]. | |||
| Squalamine | II | Monkeys | Systemic squalamine injection inhibited the |
| development of iris neovascularization and caused partial | |||
| regression of new vessels in a primate model [14] | |||
| Kahalalide F | I | Rats | MTD is 1800 μg/m2; no-adverse-effect dose |
| is 480 μg/m2/day; nephrotoxic and neurotoxic [15]. | |||
| Aplidin | II | Mice | More toxic effects with prolonged exposure [8]. |
| KRN7000b | I | N/A | N/A [4, 8] |
| Cryptophycin-52 | II | N/A | N/A [8] |
| Epothilone B | II | N/A | N/A [16] |
| LAF389c | I | N/A | N/A [4, 16] |
| ILX651a | I | N/A | N/A [4] |
| HTI286 | I | N/A | N/A [4, 17] |
N/A = not available.
aDolastatin-15 analogue.
bAgelasphin analouge (alpha-galactosylceramide).
cBengamide B analouge.