Lutetium (¹⁷⁷Lu) vipivotide tetraxetan, sold under the brand name Pluvicto, is a

radiopharmaceutical Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which ...

medication used for the treatment of prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC). Lutetium (¹⁷⁷Lu) vipivotide tetraxetan is a targeted

radioligand A radioligand is a radioactive biochemical substance (in particular, a ligand (biochemistry), ligand that is radioactive tracer, radiolabeled) that is used for diagnosis or for research-oriented study of the receptor (biochemistry), receptor system ...

therapy. The most common adverse reactions include fatigue, dry mouth, nausea, anemia, decreased appetite, and constipation. 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-177 Naturally occurring lutetium (71Lu) is composed of one stable isotope 175Lu (97.41% natural abundance) and one long-lived radioisotope, 176Lu with a half-life of 3.78 × 1010 years (2.59% natural abundance). Thirty-five radioisotopes have been ch ...

, with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium (¹⁷⁷Lu) vipivotide tetraxetan, vipivotide 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 was approved for medical use in the United States in March 2022, and in the European Union in December 2022.

History

The medication was developed by

German Cancer Research Center The German Cancer Research Center (known as the Deutsches Krebsforschungszentrum or simply DKFZ in German) is a national cancer research center based in Heidelberg, Germany. It is a member of the Helmholtz Association of German Research Centres ...

and

University Hospital Heidelberg University Hospital Heidelberg () is a university hospital in Heidelberg, Germany and is with 1,991 beds one of the largest medical centers in the country. It is closely linked to Heidelberg University Medical School (Heidelberg University Fac ...

and licensed to the small German pharmaceutical company ABX for early clinical development. In 2017 the license was acquired by

Endocyte Endocyte ( NASDAQ: ECYT) is a biopharmaceutical company established in 1996 and headquartered in West Lafayette, Indiana, a resident of the Purdue Research Park. In 2011 the company completed successfully an initial public offering (IPO). , the ...

and Endocyte itself was acquired by

Novartis Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-loc ...

in 2018. Efficacy was evaluated in VISION,. 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). All participants received a GnRH analog or had prior bilateral orchiectomy. Participants were required to have received at least one androgen receptor pathway inhibitor, and 1 or 2 prior taxane-based chemotherapy regimens. 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. The U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) granted the application for lutetium (¹⁷⁷Lu) vipivotide tetraxetan

priority review Priority review is a program of the United States Food and Drug Administration (FDA) to expedite the review process for drugs that are expected to have a particularly great impact on the treatment of a disease. The priority review voucher program ...

and

breakthrough therapy Breakthrough therapy is a United States Food and Drug Administration designation that expedites drug development that was created by Congress under Section 902 of the 9 July 2012 Food and Drug Administration Safety and Innovation Act. The FDA's "br ...

designations.

Society and culture

Legal status

On 13 October 2022, the

Committee for Medicinal Products for Human Use The Committee for Medicinal Products for Human Use (CHMP), formerly known as Committee for Proprietary Medicinal Products (CPMP), is the European Medicines Agency's committee responsible for elaborating the agency's opinions on all issues regardin ...

(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. The applicant for this medicinal product is Novartis Europharm Limited. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Lutetium (177Lu) vipivotide tetraxetan was approved for medical use in the European Union in December 2022.

References

External links

* {{DEFAULTSORT:Lutetium (177lu) Vipivotide Tetraxetan Breakthrough therapy Lutetium complexes Novartis brands Radiopharmaceuticals