Flotufolastat F-18

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C63H99FN12O25Si
Molecular Weight	1470.612
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)[Si]([18F])(C1=CC=C(C=C1)C(=O)NC[C@@H](NC(=O)CC[C@H](N2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)C(O)=O)C(=O)N[C@H](CCCCNC(=O)CCC(=O)NCCC[C@@H](NC(=O)CC[C@H](NC(=O)N[C@@H](CCC(O)=O)C(O)=O)C(O)=O)C(O)=O)C(O)=O)C(C)(C)C

InChI

InChIKey=QMGJNAVROCDAIW-MQNQVPOESA-N

InChI=1S/C63H99FN12O25Si/c1-62(2,3)102(64,63(4,5)6)39-14-12-38(13-15-39)54(89)67-34-44(69-49(80)20-18-45(60(99)100)76-32-30-74(36-52(85)86)28-26-73(35-51(83)84)27-29-75(31-33-76)37-53(87)88)55(90)70-41(57(93)94)10-7-8-24-65-46(77)21-22-47(78)66-25-9-11-40(56(91)92)68-48(79)19-16-42(58(95)96)71-61(101)72-43(59(97)98)17-23-50(81)82/h12-15,40-45H,7-11,16-37H2,1-6H3,(H,65,77)(H,66,78)(H,67,89)(H,68,79)(H,69,80)(H,70,90)(H,81,82)(H,83,84)(H,85,86)(H,87,88)(H,91,92)(H,93,94)(H,95,96)(H,97,98)(H,99,100)(H2,71,72,101)/t40-,41-,42+,43+,44-,45+/m1/s1/i64-1

HIDE SMILES / InChI

Molecular Formula	C63H99FN12O25Si
Molecular Weight	1470.612
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/37439946/|https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=907ac4a4-a088-4826-ab50-cfc31985c9d4&version=6

Flotufolastat F 18 (POSLUMA®) is an 18F-labelled radiohybrid (rh) prostate-specific membrane antigen (PSMA)-targeted imaging agent being developed by Blue Earth Diagnostics, a subsidiary of Bracco Imaging, for prostate cancer imaging. In May 2023, flotufolastat F 18 received its first approval in the USA as a radioactive diagnostic agent for positron emission tomography (PET) of PSMA positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. Flotufolastat F 18 binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized. Prostate cancer cells usually overexpress PSMA. Fluorine-18 is a beta emitting radionuclide that can be detected using positron emission tomography.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glutamate carboxypeptidase 2 2 Target ID: Q04609\|\|\|Q16305 Gene ID: 2346.0 Gene Symbol: FOLH1 Target Organism: Homo sapiens (Human) Sources: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=907ac4a4-a088-4826-ab50-cfc31985c9d4&version=6	Binding Agent 1076		4.4 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Prostate cancer 186 Sources: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=907ac4a4-a088-4826-ab50-cfc31985c9d4&version=6	Diagnostic		Approved 8583	POSLUMA Approved Use POSLUMA is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy. with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. Launch Date 2023

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193	substrate 1388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	CYP2B6 776 CYP21 1 CYP2C19 1119 CYP1A2 1197 CYP2C8 810 CYP2A6 626

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP21 1	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2023/216023Orig1s000MultidisciplineR.pdf Page: 34.0	no

PubMed

Title	Date	PubMed
Flotufolastat F 18: Diagnostic First Approval.	2023-09	37439946
Validation of 18F-rhPSMA-7 and 18F-rhPSMA-7.3 PET Imaging Results with Histopathology from Salvage Surgery in Patients with Biochemical Recurrence of Prostate Cancer.	2022-12	35393348
Utility of 18F-rhPSMA-7.3 PET for Imaging of Primary Prostate Cancer and Preoperative Efficacy in N-Staging of Unfavorable Intermediate- to Very High-Risk Patients Validated by Histopathology.	2022-09	34992154

Sample Use Guides

In Vivo Use Guide

Recommended amount of radioactivity of POSLUMA is 296 MBq (8 mCi) administered as an intravenous bolus injection. ( 2.2) Initiate imaging approximately 60 minutes after administration. Scanning should start from mid-thigh and proceed to base of skull. ( 2.4)

Route of Administration: Intravenous

In Vitro Use Guide

Flotufolastat F 18 binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 07:50:30 GMT 2025` Edited by `admin` on `Wed Apr 02 07:50:30 GMT 2025`
Record UNII	811W19E3OL
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FLOTUFOLASTAT (18F)

Preferred Name

English

Flotufolastat F-18

Official Name

English

D-LYSINE, 3-((4-(BIS(1,1-DIMETHYLETHYL)FLUORO((18F)SILYL)BENZOYL)AMINO)-N-((4S)-4-CARBOXY-1-OXO-4-(4,7,10-TRIS(CARBOXYMETHYL)-1,4,7,10-TETRAAZACYCLODODEC-1-YL)BUTYL)-D-ALANYL-N6-(3-CARBOXY-1-OXOPROPYL)-, (26->2')-AMIDE WITH N-((((1S)-1,3-DICARBOXYPROPYL)

Systematic Name

English

N2 -(N-{(4S)-4-carboxy-4-[4,7,10-tris(carboxymethyl)- 1,4,7,10-tetraaza-cyclododecan-1-yl]butanoyl}-3-[4-(ditert-butyl(18F)fluorosilyl)benzamido]-D-alanyl)-N6-[4-(N2-{N-[(L-glutamic acid-N-yl)carbonyl]- L-?-glutamyl}-Dornithin-N5-yl)-4-oxobutanoyl]-D-lys

Systematic Name

English

rhPSMA-7.3C

Code

English

FLOTUFOLASTAT F 18 [USAN]

Common Name

English

Code System Code Type Description

PUBCHEM

154572844