Stereochemistry | ABSOLUTE |
Molecular Formula | C38H73N21O10S2 |
Molecular Weight | 1048.251 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](C)NC(=O)[C@@H](CSSC[C@H](N)C(O)=O)NC(C)=O)C(=O)N[C@H](CCCNC(N)=N)C(N)=O
InChI
InChIKey=ANIAZGVDEUQPRI-ZJQCGQFWSA-N
InChI=1S/C38H73N21O10S2/c1-18(28(62)56-22(27(40)61)8-4-12-49-35(41)42)53-30(64)23(9-5-13-50-36(43)44)58-32(66)25(11-7-15-52-38(47)48)59-31(65)24(10-6-14-51-37(45)46)57-29(63)19(2)54-33(67)26(55-20(3)60)17-71-70-16-21(39)34(68)69/h18-19,21-26H,4-17,39H2,1-3H3,(H2,40,61)(H,53,64)(H,54,67)(H,55,60)(H,56,62)(H,57,63)(H,58,66)(H,59,65)(H,68,69)(H4,41,42,49)(H4,43,44,50)(H4,45,46,51)(H4,47,48,52)/t18-,19-,21+,22-,23-,24-,25-,26-/m1/s1
Etelcalcetide (formerly velcalcetide, trade name Parsabiv) is a calcimimetic drug for the treatment of secondary hyperparathyroidism in patients undergoing hemodialysis. Etelcalcetide was approved (trade name Parsabiv) for the treatment of secondary hyperparathyroidism (HPT) in adult patients with chronic kidney disease (CKD) on hemodialysis in February, 2017. Etelcalcetide is a synthetic peptide calcium-sensing receptor agonist. It allosterically modulates the calcium-sensing receptor (CaSR).
Etelcalcetide binds to the CaSR and enhances activation of the receptor by extracellular calcium. Activation of
the CaSR on parathyroid chief cells decreases PTH secretion.
Originator
Approval Year
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
Sourcing
PubMed
Patents
Sample Use Guides
Ensure corrected serum calcium is at or above the lower limit of normal prior to PARSABIV (Etelcalcetide) initiation, a PARSABIV dose increase, or re-initiation of PARSABIV therapy after a dosing interruption.
The recommended starting dose of PARSABIV is 5 mg administered by intravenous (IV) bolus injection
three times per week at the end of hemodialysis treatment.
The maintenance dose of PARSABIV is individualized and determined by titration based on parathyroid
hormone (PTH) and corrected serum calcium response. The maintenance dose is the dose that maintains PTH levels within the recommended target range and corrected
serum calcium within the normal range. The lowest maintenance dose of PARSABIV is 2.5 mg three times
per week and the highest maintenance dose of PARSABIV is 15 mg three times per week.
Administer PARSABIV only at the end of hemodialysis treatment.
If a regularly scheduled hemodialysis treatment is missed, DO NOT administer any missed doses. Resume
PARSABIV at the end of the next hemodialysis treatment at the prescribed dose. If doses of PARSABIV are
missed for more than 2 weeks, re-initiate PARSABIV at the recommended starting dose of 5 mg (or 2.5 mg
if that was the patient’s last dose).
Route of Administration:
Intravenous