Deruxtecan Property

Boiling point:

1491.1±65.0 °C(Predicted)

Density 

1.48±0.1 g/cm3(Predicted)

solubility 

DMSO:67.5(Max Conc. mg/mL);65.28(Max Conc. mM)

pka

11.18±0.40(Predicted)

InChI

InChI=1S/C52H56FN9O13/c1-3-52(73)33-19-38-48-31(23-62(38)49(70)32(33)25-75-51(52)72)47-35(14-13-30-28(2)34(53)20-36(59-48)46(30)47)57-43(67)26-74-27-60(24-39(54)63)50(71)37(18-29-10-6-4-7-11-29)58-42(66)22-56-41(65)21-55-40(64)12-8-5-9-17-61-44(68)15-16-45(61)69/h4,6-7,10-11,15-16,19-20,35,37,73H,3,5,8-9,12-14,17-18,21-27H2,1-2H3,(H2,54,63)(H,55,64)(H,56,65)(H,57,67)(H,58,66)/t35-,37-,52-/m0/s1

InChIKey

XSLGWYQNBQGZTG-MCZRLCSDSA-N

SMILES

C(N)(=O)CN(C(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)CCCCCN1C(=O)C=CC1=O)COCC(N[C@@H]1C2C3C(N=C4C5N(C(=O)C6COC(=O)[C@@](CC)(O)C=6C=5)CC4=2)=CC(F)=C(C)C=3CC1)=O

Hazard and Precautionary Statements (GHS)

Deruxtecan Chemical Properties,Usage,Production

Uses

Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.

Indications

By Deruxtecan Preparation Trastuzumab deruxtecan drug is approved by the FDA for the treatment of patients with any HER2-positive advanced solid tumour (e.g., breast, gastric, and GOJ adenocarcinomas) and only after the patient has previously received other advanced treatments.

Mechanism of action

Deruxtecan is attached to the antibody by a peptide linker. After trastuzumab deruxtecan binds to HER2 found on malignant cells, it is internalized and linker cleavage occurs through the actions of lysosomal enzymes. After it is released through cleavage, DXd causes targeted DNA damage and apoptosis in cancer cells, due to the ability to cross cell membranes.

Side effects

The most common side effects of Deruxtecan (Trastuzumab deruxtecan) include: nausea, vomiting, diarrhoea, fatigue, hair loss, increased risk of infections (low white blood cell counts, red blood cell counts, and platelet counts), breathlessness, coughing, headache, bone or muscle pain, mouth ulcers, loss of appetite, weight loss, heart problems, liver or skin changes, low potassium levels. All of these side effects may not always occur at the same time and will vary from person to person. Serious adverse reactions include: interstitial lung disease/pneumonia, serious impairment of heart function and allergic reactions. Special care should be taken to contact your doctor in case of any serious adverse reactions.