Lutetium Lu 177 vipivotide tetraxetan

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PSMA-617 Lu-177.png

2D chemical structure of 1703749-62-5

177Lu vipivotide tetraxetan -177LU-PSMA-617.svg

ChemSpider 2D Image | (~177~Lu)Lutetium 2,2',2''-[10-(2-{[(trans-4-{[(2S)-1-{[(5S)-5-carboxy-5-({[(1S)-1,3-dicarboxypropyl]carbamoyl}amino)pentyl]amino}-3-(2-naphthyl)-1-oxo-2-propanyl]carbamoyl}cyclohexyl)methyl]amino}-2- oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl]triacetate (non-preferred name) | C49H68177LuN9O16

177Lu vipivotide tetraxetan -177LU-PSMA-617.svg

Lutetium Lu 177 vipivotide tetraxetan

FDA APPROVED 2022/3/23, Pluvicto

To treat prostate-specific membrane antigen-positive metastatic castration-resistant prostate cancer following other therapies

Formula
C49H65N9O16. Lu. 3H
CAS
1703749-62-5
Mol weight
1214.0819
Antineoplastic, Radioactive agent
  Disease
Prostate cancer (PSMA positive)

ルテチウム(177Lu)ビピボチドテトラキセタン;

UNII-G6UF363ECX, WHO 11429

G6UF363ECX

177Lu-Psma-617

Vipivotide tetraxetan Lu-177

177Lu-Labeled PSMA-617

2-[4-[2-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxypropyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]cyclohexyl]methylamino]-2-oxoethyl]-7,10-bis(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate;lutetium-177(3+)

(177Lu)Lutetium 2,2′,2′‘-[10-(2-{[(trans-4-{[(2S)-1-{[(5S)-5-carboxy-5-({[(1S)-1,3-dicarboxypropyl]carbamoyl}amino)pentyl]amino}-3-(2-naphthyl)-1-oxo-2-propanyl]carbamoyl}cyclohexyl)methyl]amino}-2- oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl]triacetate (non-preferred name)
1983157-55-6 [RN]
PSMA-617 LU-177

Lutetium Lu 177 Vipivotide Tetraxetan is a radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 vipivotide tetraxetanvipivotide tetraxetan targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.

Lutetium (177Lu) vipivotide tetraxetan, sold under the brand name Pluvicto, is a radiopharmaceutical medication used for the treatment of prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC).[2] Lutetium (177Lu) vipivotide tetraxetan is a targeted radioligand therapy.[2][3]

The most common adverse reactions include fatigue, dry mouth, nausea, anemia, decreased appetite, and constipation.[2]

Lutetium (177Lu) vipivotide tetraxetan is a radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells.[4] Upon intravenous administration of lutetium Lu 177 vipivotide tetraxetan, vipivotide tetraxetan targets and binds to PSMA-expressing tumor cells.[4] Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation.[4] PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.[4]

Lutetium (177Lu) vipivotide tetraxetan was approved for medical use in the United States in March 2022.[2][5]

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History[edit]

Efficacy was evaluated in VISION (NCT03511664), 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).[2] All participants received a GnRH analog or had prior bilateral orchiectomy.[2] Participants were required to have received at least one androgen receptor pathway inhibitor, and 1 or 2 prior taxane-based chemotherapy regimens.[2] Participants received lutetium (177Lu) vipivotide tetraxetan 7.4 GBq (200 mCi) every 6 weeks for up to a total of 6 doses plus BSoC or BSoC alone.[2]

The U.S. Food and Drug Administration granted the application for lutetium (177lu) vipivotide tetraxetan priority review and breakthrough therapy designations.[2]

References

  1. ^ “Highlights of prescribing information: PLUVICTOTM (lutetium Lu 177 vipivotide tetraxetan) injection, for intravenous use” (PDF)Advanced Accelerator Applications USA, Inc. Novartis. March 2022.
  2. Jump up to:a b c d e f g h i j “FDA approves Pluvicto for metastatic castration-resistant prostate can”U.S. Food and Drug Administration. 23 March 2022. Retrieved 23 March 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ Neels OC, Kopka K, Liolios C, Afshar-Oromieh A (December 2021). “Radiolabeled PSMA Inhibitors”Cancers13 (24): 6255. doi:10.3390/cancers13246255PMC 8699044PMID 34944875.
  4. Jump up to:a b c d “Lutetium Lu 177 Vipivotide Tetraxetan (Code C148145)”. NCI Thesaurus. 28 February 2022. Retrieved 23 March 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  5. ^ “Novartis Pluvicto approved by FDA as first targeted radioligand therapy for treatment of progressive, PSMA positive metastatic castration-resistant prostate cancer” (Press release). Novartis. 23 March 2022. Retrieved 23 March 2022.

External links

Lutetium (177Lu) vipivotide tetraxetan
177Lu vipivotide tetraxetan -177LU-PSMA-617.svg
Clinical data
Trade names Pluvicto
Other names 177Lu-PSMA-617, Lutetium Lu 177 vipivotide tetraxetan (USAN US)
License data
Routes of
administration
Intravenous
Drug class Radiopharmaceutical
ATC code
  • None
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
3D model (JSmol)

////////////Lutetium Lu 177 vipivotide tetraxetan, ルテチウム(177Lu)ビピボチドテトラキセタン, FDA 2022, APPROVALS 2022, PROSTRATE CANCER, WHO 11429

C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)[O-])CC(=O)[O-])CC(=O)[O-])C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCCC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O.[Lu+3]

 

Vipivotide tetraxetan Chemical Structure

Vipivotide tetraxetan (Synonyms: PSMA-617)

CAS No. : 1702967-37-0

Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.

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