Table 2.
Compound screening results in µP-hPST. The Cmax values of each compound were mainly acquired from U.S. Food and Drug Administration website, European Medicines Agency website or published journals unless otherwise noted. The full list could be found in Supplementary Table S1. NON: Non-teratogen, TER: Teratogen, NA: not applicable.
| Drug name | IC25aHDF (µg/ml) | IC25H9 (µg/ml) | Cmax (µg/ml) | LDC (µg/ml) | Step1: Is LDC <= IC25 aHDF & IC25H9? | Step 2: Is LDC <= 10 Cmax? | Teratogenicity in µP-hPST | Teratogenicity in other in vitro assays | In vivo teratogenicity |
|---|---|---|---|---|---|---|---|---|---|
| Acetaminophen | 40 | 171 | 24 | 160 | N | - | NON | NON6 | NON |
| Acyclovir | 285 | 267 | 5.65 | 60 | Y | N | NON | NON6, 7 | NON |
| Amoxicillin | >1000 | >1000 | 14.4 | 150 | Y | N | NON | NON6 | NON |
| Ascorbic acid | 63 | 105 | 156 | 80 | N | — | NON | NON6 | NON |
| Caffeine | 129 | 85.4 | 10 | 130 | N | — | NON | NON6, 7 | NON |
| Diphenhydramine | 31.4 | 2.4 | 0.06 | 2.4 | Y | N | NON | NON6 | NON |
| Doxylamine | 45 | 87 | 0.12 | 45 | Y | N | NON | NON6 | NON |
| Esomeprazole | 42.1 | 38.9 | 1.62 | 45 | N | — | NON | NON7 | NON |
| Folic acid | 894 | 888 | 0.27 | 900 | N | — | NON | NON6 | NON |
| Isoniazid | 488 | 370 | 3.09 | 500 | N | — | NON | NON6 | NON |
| Loratadine | 3.2 | 24 | 0.04 | 4 | N | — | NON | NON6 | NON |
| Metoclopramide | 154 | 162 | 0.04 | 120 | Y | N | NON | NON6 | NON |
| Methyldopa | 15.9 | 23.2 | 7.5 | 25 | N | — | NON | NON7 | NON |
| Sitagliptin | 77.1 | 359 | 0.39 | >360 | N | — | NON | NON6 | NON |
| Thiamine | >1000 | >1000 | 0.11 | 1000 | Y | N | NON | NON6 | NON |
| 5-Fluorouracil | 0.16 | 0.15 | 48.4 | 0.025 | Y | Y | TER | TER6, 7 | TER |
| Bosentan | 19.9 | 43.8 | 8.17 | 16 | Y | Y | TER | NON6 | TER |
| Busulfan | 19.2 | 0.5 | 1.22 | 0.2 | Y | Y | TER | TER6 | TER |
| Carbamazepine | 28 | 21 | 11 | 10 | Y | Y | TER | TER6 | TER |
| Diethylstilbestrol | 6.1 | 8.8 | 0.0056 | 5 | Y | N | NON | TER7 | TER |
| Diphenylhydantoin | 140 | 56 | 20 | 50 | Y | Y | TER | NON6 | TER |
| Doxorubicin | 0.003 | 0.0002 | 0.37 | 0.00015 | Y | Y | TER | TER7 | TER |
| Furosemide | 30 | 362 | 400 | 30 | Y | Y | TER | NON28 | TER |
| Gefitinib | 1.66 | 4.6 | 0.93 | 0.9 | Y | Y | TER | TER7 | TER |
| Imatinib | 2.7 | 19.5 | 1.56 | 0.75 | Y | Y | TER | TER7 | TER |
| Lovastatin | 0.68 | 0.30 | 0.01 | 0.01 | Y | Y | TER | NON6 | TER |
| Methimazole | >1000 | 252 | 0.3 | 1.5 | Y | Y | TER | NA | TER |
| Sunitinib | 0.18 | 0.89 | 0.03 | 0.15 | Y | Y | TER | TER7 | TER |
| Vandetanib | 1.1 | 0.3 | 0.4 | 0.3 | Y | Y | TER | TER7 | TER |
| Ziprasidone | 2.7 | 14.4 | 0.2 | 1.25 | Y | Y | TER | TER7 | TER |