Lutetium (177Lu) Vipivotide Tetraxetan

Lutetium (¹⁷⁷Lu) vipivotide tetraxetan

Names
Trade names	Pluvicto
Other names	177Lu-PSMA-617, Lutetium Lu 177 vipivotide tetraxetan (USAN US)
Clinical data
Drug class	Radiopharmaceutical
Main uses	Prostate cancer[1]
Side effects	Tiredness, dry mouth, nausea, low hemoglobin, decreased appetite, constipation[1]
Routes of use	Intravenous
Legal
License data	US DailyMed: Pluvicto
Legal status	CA: ℞-only [2] US: ℞-only [1][3]
Chemical and physical data
3D model (JSmol)	Interactive image
SMILES [177Lu+3].OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]3CC[C@@H](CNC(=O)CN4CCN(CC(=O)[O-])CCN(CC(=O)[O-])CCN(CC(=O)[O-])CC4)CC3)C(=O)O)C(=O)O
InChI InChI=1S/C49H71N9O16.Lu/c59-40(28-55-17-19-56(29-42(62)63)21-23-58(31-44(66)67)24-22-57(20-18-55)30-43(64)65)51-27-32-8-12-35(13-9-32)45(68)52-39(26-33-10-11-34-5-1-2-6-36(34)25-33)46(69)50-16-4-3-7-37(47(70)71)53-49(74)54-38(48(72)73)14-15-41(60)61;/h1-2,5-6,10-11,25,32,35,37-39H,3-4,7-9,12-24,26-31H2,(H,50,69)(H,51,59)(H,52,68)(H,60,61)(H,62,63)(H,64,65)(H,66,67)(H,70,71)(H,72,73)(H2,53,54,74);/q;+3/p-3/t32-,35-,37-,38-,39-;/m0./s1/i;1+2 Key:RSTDSVVLNYFDHY-BGOLSCJMSA-K

Lutetium (¹⁷⁷Lu) vipivotide tetraxetan, sold under the brand name Pluvicto, is a radioactive medication used to treat metastatic castration-resistant prostate cancer (mCRPC) that is prostate-specific membrane antigen (PSMA)-positive.^[1] It is given by injection into a vein.^[4]

Common side effects include tiredness, dry mouth, nausea, low hemoglobin, decreased appetite, and constipation.^[1] Other side effects may include radiation exposure, bone marrow suppression, infertility, and kidney problems.^[1] Use by males with pregnant partners may harm the baby.^[1] Vipivotide tetraxetan binds to PSMA-expressing tumor cells while the attached 177Lu destroys the cells by beta particle radiation.^[4]

Lutetium (¹⁷⁷Lu) vipivotide tetraxetan was approved for medical use in the United States in 2022.^[1] In October 2022, Europe recommended its approval.^[5] In the United States it costs about 45,000 USD per dose as of 2022.^[6]

Medical uses[edit | edit source]

Dosage[edit | edit source]

It is generally give at a dose of 7.4 GBq (200 mCi) every 6 weeks for up to a total of 6 doses plus BSoC or BSoC alone.^[3]

History[edit | edit source]

The medication was developed by German Cancer Research Center and University Hospital Heidelberg and licensed to the small German pharmaceutical company ABX for early clinical development. In 2017 the license was acquired by Endocyte^[7] and Endocyte itself was acquired by Novartis in 2018.^[8]

Efficacy was evaluated in VISION,^[9] a randomized (2:1), multicenter, open-label trial that evaluated lutetium (¹⁷⁷Lu) vipivotide tetraxetan plus best standard of care (BSoC) (n=551) or BSoC alone (n=280) in men with progressive, prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC).^[3] All participants received a GnRH analog or had prior bilateral orchiectomy.^[3] Participants were required to have received at least one androgen receptor pathway inhibitor, and 1 or 2 prior taxane-based chemotherapy regimens.^[3]

The U.S. Food and Drug Administration (FDA) granted the application for lutetium (¹⁷⁷Lu) vipivotide tetraxetan priority review and breakthrough therapy designations.^[3]

Society and culture[edit | edit source]

Legal status[edit | edit source]

On 13 October 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Pluvicto, intended for the treatment of prostate cancer.^[10] The applicant for this medicinal product is Novartis Europharm Limited.^[10]

References[edit | edit source]

External links[edit | edit source]

• "Lutetium lu 177 vipivotide tetraxetan". Drug Information Portal. U.S. National Library of Medicine. Archived from the original on 2022-08-15. Retrieved 2022-10-20.