Piflufolastat F-18

Piflufolastat F-18
Clinical data
Trade names	Pylarify, Pylclari
Other names	18F-DCFPyL
AHFS/Drugs.com	Micromedex Detailed Consumer Information
License data	US DailyMed: Piflufolastat;
Routes of; administration	Intravenous
ATC code	V09IX16 (WHO) ;
Legal status
Legal status	US: ℞-only; EU: Rx-only;
Identifiers
CAS Number	1207181-29-0;
PubChem CID	52950901;
DrugBank	DB14805;
ChemSpider	32702072;
UNII	3934EF02T7;
KEGG	D12132;
ChEMBL	ChEMBL4297334;
Chemical and physical data
Formula	C18H23[18F]N4O8
Molar mass	441.4 g/mol
3D model (JSmol)	Interactive image;
	SMILES OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)C1=CC=C([18F])N=C1)C(O)=O)C(O)=O;
	InChI InChI=1S/C18H23FN4O8/c19-13-6-4-10(9-21-13)15(26)20-8-2-1-3-11(16(27)28)22-18(31)23-12(17(29)30)5-7-14(24)25/h4,6,9,11-12H,1-3,5,7-8H2,(H,20,26)(H,24,25)(H,27,28)(H,29,30)(H2,22,23,31)/t11-,12-/m0/s1/i19-1; Key:OLWVRJUNLXQDSP-MVBOSPHXSA-N;

Piflufolastat F-18, sold under the brand name Pylarify among others, is a radioactive diagnostic agent used for positron emission tomography (PET) imaging.^[1]^[4]^[5] It is given by intravenous injection.^[1]^[4]

The most common adverse reactions include headache, altered taste, and fatigue.^[4]

Piflufolastat F-18 was approved for medical use in the United States in May 2021.^[1]^[6]^[4] It is the second PSMA-targeted PET imaging drug approved by the U.S. Food and Drug Administration (FDA).^[4] The first approved PSMA-targeted PET imaging drug is Ga 68 PSMA-11.^[4]

Medical uses

Piflufolastat F-18 is indicated for people with suspected prostate cancer metastasis (when cancer cells spread from the place where they first formed to another part of the body) who are potentially curable by surgery or other therapy.^[1]^[4] Piflufolastat F-18 is also indicated for people with suspected prostate cancer recurrence based on elevated serum prostate-specific antigen (PSA) levels.^[1]^[4]

History

The safety and efficacy of piflufolastat F-18 were evaluated in two prospective clinical trials (trial 1/NCT02981368 and trial 2/NCT03739684) with a total of 593 men with prostate cancer who each received one injection of piflufolastat F-18.^[4]^[7] In the first trial, a cohort of 268 participants with biopsy-proven prostate cancer underwent PET/CT scans performed with piflufolastat F-18.^[4] These participants were candidates for surgical removal of the prostate gland and pelvic lymph nodes and were considered at higher risk for metastasis.^[4] Among the participants who proceeded to surgery, those with positive readings in the pelvic lymph nodes on piflufolastat F-18 PET had a clinically important rate of metastatic cancer confirmed by surgical pathology.^[4]

The second trial enrolled 208 participants who had rising serum prostate-specific antigen levels after initial prostate surgery or other definitive therapy, and thus had biochemical evidence of recurrent prostate cancer.^[4] Prior to a single piflufolastat F-18 PET/CT scan, all of these participants had baseline conventional imaging performed that did not show definite spread of prostate cancer.^[4] Piflufolastat F-18 PET detected at least one positive lesion in at least one body region (bone, prostate bed, pelvic lymph node, other lymph nodes, or soft tissue) in 60% of these participants.^[4] In participants with positive piflufolastat F-18 PET readings who had correlative tissue pathology from biopsies, results from baseline or follow-up imaging by conventional methods, or serial PSA levels available for comparison, local recurrence or metastasis of prostate cancer was confirmed in an estimated 85% to 87% of cases, depending on the reader.^[4] Thus, the second trial demonstrated that piflufolastat F-18 PET can detect sites of disease in participants with biochemical evidence of recurrent prostate cancer, thereby providing important information that may impact the approach to therapy.^[4]

Trial 1 included two groups of participants, some with recently diagnosed prostate cancer and others with suspicious findings on standard tests.^[7] Trial 2 included participants who were treated for prostate cancer before, but there was suspicion that the cancer was spreading because of rising prostate-specific antigen.^[7] Participants in trial 2 and the recently diagnosed participants in trial 1 were studied for effectiveness of piflufolastat F-18, and all participants were studied for safety.^[7] Trial 1 was conducted at eight sites in the United States and two sites in Canada, and trial 2 was conducted at thirteen sites in the United States and one site in Canada.^[7] The number of participants representing efficacy findings may differ from the number of participants representing safety findings due to different pools of study participants analyzed for efficacy and safety.^[7]

The US Food and Drug Administration (FDA) granted approval of Pylarify to Progenics Pharmaceuticals, Inc.^[4]

References

^ ^a ^b ^c ^d ^e ^f "Pylarify- piflufolastat f-18 injection". DailyMed. Archived from the original on 13 September 2021. Retrieved 12 September 2021.
^ "Pylclari EPAR". European Medicines Agency. 28 July 2023. Retrieved 4 August 2023.
^ "Pylclari". Union Register of medicinal products. 25 July 2023. Retrieved 4 August 2023.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r "FDA approves PSMA-targeted imaging drug for men with prostate cancer". U.S. Food and Drug Administration (FDA). 27 May 2021. Archived from the original on 11 September 2021. Retrieved 12 September 2021. This article incorporates text from this source, which is in the public domain.
^ Keam SJ (September 2021). "Piflufolastat F 18: Diagnostic First Approval". Molecular Diagnosis & Therapy. 25 (5): 647–656. doi:10.1007/s40291-021-00548-0. PMID 34292532. S2CID 236174886.
^ "Drug Approval Package: Pylarify". U.S. Food and Drug Administration (FDA). 9 June 2021. Archived from the original on 13 September 2021. Retrieved 12 September 2021.
^ ^a ^b ^c ^d ^e ^f "Drug Trials Snapshots: Pylarify". U.S. Food and Drug Administration. 26 May 2021. Archived from the original on 28 July 2023. Retrieved 28 July 2023. This article incorporates text from this source, which is in the public domain.

This article incorporates public domain material from the United States Department of Health and Human Services

External links

"SDS Data Sheet" (PDF).
Clinical trial number NCT02981368 for "Study of 18F-DCFPyL PET/CT Imaging in Patients With Prostate Cancer (OSPREY)" at ClinicalTrials.gov
Clinical trial number NCT03739684 for "Study of 18F-DCFPyL PET/CT Imaging in Patients With Suspected Recurrence of Prostate Cancer (CONDOR)" at ClinicalTrials.gov

[Pylarify_FDA_label-1] ^ ^a ^b ^c ^d ^e ^f "Pylarify- piflufolastat f-18 injection". DailyMed. Archived from the original on 13 September 2021. Retrieved 12 September 2021.

[Pylclari_EPAR-2] "Pylclari EPAR". European Medicines Agency. 28 July 2023. Retrieved 4 August 2023.

[3] "Pylclari". Union Register of medicinal products. 25 July 2023. Retrieved 4 August 2023.

[FDA_Pylarify-4] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r "FDA approves PSMA-targeted imaging drug for men with prostate cancer". U.S. Food and Drug Administration (FDA). 27 May 2021. Archived from the original on 11 September 2021. Retrieved 12 September 2021. This article incorporates text from this source, which is in the public domain.

[pmid34292532-5] Keam SJ (September 2021). "Piflufolastat F 18: Diagnostic First Approval". Molecular Diagnosis & Therapy. 25 (5): 647–656. doi:10.1007/s40291-021-00548-0. PMID 34292532. S2CID 236174886.

[6] "Drug Approval Package: Pylarify". U.S. Food and Drug Administration (FDA). 9 June 2021. Archived from the original on 13 September 2021. Retrieved 12 September 2021.

[Pylarify_FDA_snapshot-7] ^ ^a ^b ^c ^d ^e ^f "Drug Trials Snapshots: Pylarify". U.S. Food and Drug Administration. 26 May 2021. Archived from the original on 28 July 2023. Retrieved 28 July 2023. This article incorporates text from this source, which is in the public domain.

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