Synonym
Etavopivat; FT-4202; FT 4202; FT4202;
IUPAC/Chemical Name
(2S)-1-[5-(2,3-dihydro[1,4]dioxino[2,3-b]pyridine-7-sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]-3-hydroxy-2-phenylpropan-1-one
InChi Key
KZFFYEPYCVDOGE-LJQANCHMSA-N
InChi Code
InChI=1S/C22H23N3O6S/c26-14-19(15-4-2-1-3-5-15)22(27)24-10-16-12-25(13-17(16)11-24)32(28,29)18-8-20-21(23-9-18)31-7-6-30-20/h1-5,8-9,19,26H,6-7,10-14H2/t19-/m1/s1
SMILES Code
O=C(N1CC(CN(S(=O)(C2=CN=C(OCCO3)C3=C2)=O)C4)=C4C1)[C@@H](C5=CC=CC=C5)CO
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
457.50
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Schroeder P, Fulzele K, Forsyth S, Ribadeneira MD, Guichard S, Wilker E, Marshall CG, Drake A, Fessler R, Konstantinidis DG, Seu KG, Kalfa TA. Etavopivat, a Pyruvate Kinase Activator in Red Blood Cells, for the Treatment of Sickle Cell Disease. J Pharmacol Exp Ther. 2022 Mar;380(3):210-219. doi: 10.1124/jpet.121.000743. Epub 2022 Jan 14. PMID: 35031585.
2: Fattizzo B, Motta I. Rise of the planet of rare anemias: An update on emerging treatment strategies. Front Med (Lausanne). 2023 Jan 9;9:1097426. doi: 10.3389/fmed.2022.1097426. PMID: 36698833; PMCID: PMC9868867.
3: Forsyth S, Schroeder P, Geib J, Vrishabhendra L, Konstantinidis DG, LaSalvia K, Ribadeneira MD, Wu E, Kelly P, Kalfa TA. Safety, Pharmacokinetics, and Pharmacodynamics of Etavopivat (FT-4202), an Allosteric Activator of Pyruvate Kinase-R, in Healthy Adults: A Randomized, Placebo-Controlled, Double-Blind, First-in-Human Phase 1 Trial. Clin Pharmacol Drug Dev. 2022 May;11(5):654-665. doi: 10.1002/cpdd.1058. Epub 2022 Jan 12. PMID: 35019238; PMCID: PMC9306898.
4: Matte A, Federti E, De Franceschi L. Erythrocyte pyruvate kinase activation in red cell disorders. Curr Opin Hematol. 2023 May 1;30(3):93-98. doi: 10.1097/MOH.0000000000000758. Epub 2023 Feb 9. PMID: 36853806.
5: Chou ST, Hendrickson JE, Fasano RM. Transfusion therapy for sickle cell disease: what's new? Blood Adv. 2023 Jun 13;7(11):2551-2553. doi: 10.1182/bloodadvances.2022009283. PMID: 36562748; PMCID: PMC10242629.
