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[0042] In step 4), Alloc in Fmoc-Lys(Alloc)-OH is removed twice using 0.1-0.3 equivalents of Pd(PPh 3 ) 4 and 5-10 equivalents of morpholine or phenylsilane for 10-30 min each time, wherein CH 2 Cl 2 is used as a solvent in the removal
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The decision to terminate the clinical development of Lotiglipron was based on the pharmacokinetic data from the clinical Phase 1 drug-drug interaction studies (NCT05671653 and NCT05788328), as well as the laboratory measurements of elevated transaminases in these Phase 1 studies and the ongoing Phase 2 study (NCT05579977)
