Delving into the Latest Updates on BAY-867548 with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms

68Ga-Bombesin, Bombesin (68Ga) labelled, Gallium-68-bombesin

+ [9]

Target

GRPR

Action

modulators

Mechanism

GRPR modulators(Gastrin releasing peptide receptor modulators)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic CancerAdenocarcinoma of prostateMetastatic Prostate Carcinoma

Inactive Indication

Recurrent Prostate Carcinoma

Originator Organization

University of Bern

Active Organization

Lantheus Holdings, Inc.

Bayer AG

Stanford University

Inactive Organization

Life Molecular Imaging Ltd.

National Institutes of Health

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC78H115GaN20O19

InChIKeyHPQFXKMKTOABLV-ZQSXMSGHSA-K

CAS Registry1444870-03-4

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Sequence Code 19351754

The main goal of this phase II clinical trial is to define a novel approach of staging prostate cancer (PCa) patients by using a fully integrated positron emission tomography/ magnetic resonance imaging (PET/MRI) system with 68Ga-prostate specifica membrane antigen (PSMA) and 68Ga-RM2 (bombesin antagonist).
50 patients with biopsy proven PCa will be studied by PET/MRI with 68Ga-PSMA and with 68Ga-RM2 and then will undergo prostatectomy and pelvic lymphadenectomy.

Start Date09 Sep 2020

Sponsor / Collaborator

IRCCS San Raffaele Roma Srl

NCT05806853

/ CompletedPhase 2IIT

Phase II Prospective Monocentric Study on Prostate Cancer Restaging by Using PET/MR With Innovative Radiotracers

The overall goal is to provide an innovative approach to restage patients with biochemical recurrence of prostate cancer by using hybrid PET/MR with innovative radiotracers (68Ga-PSMA and 68Ga-RM2)

Start Date03 Jun 2020

Sponsor / Collaborator

Ospedale San Raffaele Srl

100 Clinical Results associated with BAY-867548

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100 Translational Medicine associated with BAY-867548

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100 Patents (Medical) associated with BAY-867548

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32

Literatures (Medical) associated with BAY-867548

01 Sep 2024·European Journal of Nuclear Medicine and Molecular Imaging

Development and evaluation of albumin binder-conjugated heterodimeric radiopharmaceuticals targeting integrin αvβ3 and CD13 for cancer therapy

Article

Author: Lv, Xiaoying ; Lan, Xiaoli ; Shan, Changyu ; An, Rui ; Long, Yu ; Gai, Yongkang ; Zeng, Dexing ; Song, Xiangming ; Yang, Biao

PURPOSEThe advancement of heterodimeric tracers, renowned for their high sensitivity, marks a significant trend in the development of radiotracers for cancer diagnosis. Our prior work on [⁶⁸Ga]Ga-HX01, a heterodimeric tracer targeting CD13 and integrin α_vβ₃, led to its approval for phase I clinical trials by the China National Medical Production Administration (NMPA). However, its fast clearance and limited tumor retention pose challenges for broader clinical application in cancer treatment. This study aims to develop a new radiopharmaceutical with increased tumor uptake and prolonged retention, rendering it a potential therapeutic candidate.METHODSNew albumin binder-conjugated compounds were synthesized based on the structure of HX01. In vitro and in vivo evaluation of these new compounds were performed after labelling with ⁶⁸Ga. Small-animal PET/CT imaging were conducted at different time points at 0.5-6 h post injection (p.i.) using BxPC-3 xenograft mice models. The one with the best imaging performance was further radiolabeled with ¹⁷⁷Lu for small-animal SPECT/CT and ex vivo biodistribution investigation.RESULTSWe have synthesized novel albumin binder-conjugated compounds, building upon the structure of HX01. When radiolabeled with ⁶⁸Ga, all compounds demonstrated improved pharmacokinetics (PK). Small-animal PET/CT studies revealed that these new albumin binder-conjugated compounds, particularly [⁶⁸Ga]Ga-L6, exhibited significantly enhanced tumor accumulation and retention compared with [⁶⁸Ga]Ga-L0 without an albumin binder. [⁶⁸Ga]Ga-L6 outperformed [⁶⁸Ga]Ga-L7, a compound developed using a previously reported albumin binder. Furthermore, [¹⁷⁷Lu]Lu-L6 demonstrated rapid clearance from normal tissues, high tumor uptake, and prolonged retention in small-animal SPECT/CT and biodistribution studies, positioning it as an ideal candidate for radiotherapeutic applications.CONCLUSIONA new integrin α_vβ₃ and CD13 targeting compound was screened out. This compound bears a novel albumin binder and exhibits increased tumor uptake and prolonged tumor retention in BxPC-3 tumors and low background in normal organs, making it a perfect candidate for radiotherapy when radiolabeled with ¹⁷⁷Lu.

01 Apr 2024·The Lancet Oncology

68Ga-RM2 PET–MRI versus MRI alone for evaluation of patients with biochemical recurrence of prostate cancer: a single-centre, single-arm, phase 2/3 imaging trial

Article

Author: Liang, Tie ; Song, Hong ; Moradi, Farshad ; Davidzon, Guido A ; Vasanawala, Shreyas ; Iagaru, Andrei ; Duan, Heying ; Loening, Andreas M ; Brooks, James D ; Srinivas, Sandy ; Hancock, Steven

BACKGROUNDNational Comprehensive Cancer Network guidelines include prostate-specific membrane antigen (PSMA)-targeted PET for detection of biochemical recurrence of prostate cancer. However, targeting a single tumour characteristic might not be sufficient to reflect the full extent of disease. Gastrin releasing peptide receptors (GRPR) have been shown to be overexpressed in prostate cancer. In this study, we aimed to evaluate the diagnostic performance of the GRPR-targeting radiopharmaceutical ⁶⁸Ga-RM2 in patients with biochemical recurrence of prostate cancer.METHODSThis single-centre, single-arm, phase 2/3 trial was done at Stanford University (USA). Adult patients (aged ≥18 years) with biochemical recurrence of prostate cancer, a Karnofsky performance status of 50 or higher, increasing prostate-specific antigen concentration 0·2 ng/mL or more after prostatectomy or 2 ng/mL or more above nadir after radiotherapy, and non-contributory conventional imaging (negative CT or MRI, and bone scan) were eligible. All participants underwent ⁶⁸Ga-RM2 PET-MRI. The primary outcome was the proportion of patients with PET-positive findings on ⁶⁸Ga-RM2 PET-MRI compared with MRI alone after initial therapy, at a per-patient and per-lesion level. The primary outcome would be considered met if at least 30% of patients had one or more lesions detected by ⁶⁸Ga-RM2 PET-MRI and the detection by ⁶⁸Ga-RM2 PET-MRI was significantly greater than for MRI. Each PET scan was interpreted by three independent masked readers using a standardised evaluation criteria. This study is registered with ClinicalTrials.gov, NCT02624518, and is complete.FINDINGSBetween Dec 12, 2015, and July 27, 2021, 209 men were screened for eligibility, of whom 100 were included in analyses. Median follow-up was 49·3 months (IQR 36·7-59·2). The primary endpoint was met; ⁶⁸Ga-RM2 PET-MRI was positive in 69 (69%) patients and MRI alone was positive in 40 (40%) patients (p<0·0001). In the per-lesion analysis ⁶⁸Ga-RM2 PET-MRI showed significantly higher detection rates than MRI alone (143 vs 96 lesions; p<0·0001). No grade 1 or worse events were reported.INTERPRETATION⁶⁸Ga-RM2 PET-MRI showed better diagnostic performance than MRI alone in patients with biochemical recurrence of prostate cancer. Further prospective comparative studies with PSMA-targeted PET are needed to gain a better understanding of GRPR and PSMA expression patterns in these patients.FUNDINGThe US Department of Defense.

11 Sep 2023·Pharmaceuticals (Basel, Switzerland)

Investigation of the Effect on the Albumin Binding Moiety for the Pharmacokinetic Properties of ⁶⁸Ga-, ^205/206Bi-, and ¹⁷⁷Lu-Labeled NAPamide-Based Radiopharmaceuticals.

Article

Author: Szabó, Judit P ; Szikra, Dezső ; Szücs, Dániel ; Gyuricza, Barbara ; Tóth, Imre ; Fekete, Anikó ; Képes, Zita ; Trencsényi, György ; Arató, Viktória

Although radiolabeled alpha-melanocyte stimulating hormone-analogue NAPamide derivatives are valuable melanoma-specific diagnostic probes, their rapid elimination kinetics and high renal uptake may preclude them from being used in clinical settings. We aimed at improving the pharmacokinetics of radiolabeled DOTA-NAPamide compounds by incorporating a 4-(p-iodo-phenyl)-butanoic acid (IPB) into the molecules. Followed by ⁶⁸Ga-, ^205/206Bi-, and ¹⁷⁷Lu-labelling, the radiopharmaceuticals ([⁶⁸Ga]Ga-DOTA-IPB-NAPamide, [^205/206Bi]Bi-DOTA-IPB-NAPamide, [¹⁷⁷Lu]Lu-DOTA-IPB-NAPamide) were characterized in vitro. To test the imaging behavior of the IPB-containing probes, B16F10 tumor-bearing C57BL/6 mice were subjected to in vivo microPET/microSPECT/CT imaging and ex vivo biodistribution studies. All tracers were stable in vitro, with radiochemical purity exceeding 98%. The use of albumin-binding moiety lengthened the in vivo biological half-life of the IPB-carrying radiopharmaceuticals, resulting in elevated tumor accumulation. Both [⁶⁸Ga]Ga-DOTA-IPB-NAPamide (5.06 ± 1.08 %ID/g) and [^205/206Bi]Bi-DOTA-IPB-NAPamide (4.50 ± 0.98 %ID/g) exhibited higher B16F10 tumor concentrations than their matches without the albumin-binding residue ([⁶⁸Ga]Ga-DOTA-NAPamide and [^205/206Bi]Bi-DOTA-NAPamide: 1.18 ± 0.27 %ID/g and 3.14 ± 0.32; respectively), however; the large amounts of off-target radioactivity do not confirm the benefits of half-life extension for short-lived isotopes. Enhanced [¹⁷⁷Lu]Lu-DOTA-IPB-NAPamide tumor uptake even 24 h post-injection proved the advantage of IPB-based prolonged circulation time regarding long-lived radionuclides, although the significant background noise must be addressed in this case as well.

100 Deals associated with BAY-867548

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Adenocarcinoma of prostate	Phase 3	United States	Stanford University	16 Nov 2015
Prostatic Cancer	Phase 3	-	Bayer AG	-
Recurrent Prostate Carcinoma	Phase 2	France	-	25 Apr 2018
Metastatic Prostate Carcinoma	Phase 2	United States	Lantheus Holdings, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02624518 (CTgov)	Phase 2/3	Adenocarcinoma of prostate	122	Positron Emission Tomography+68Ga-RM2	qymzefwubz(srfstqhpxt) = sqqorwjoml pcglsayrcq (itrplarllm, truiqefcmi - cqwndxzlmh) View more	-	10 Apr 2023
SNMMI2022	Not Applicable	Prostatic Cancer	-	68Ga-PSMA1168Ga-RM2A11 (68Ga-RM2 PET/MRI)	(kqwwxjnwwm) = byokjxqubn fohehcnymw (qdvprqlsvm ) View more	-	08 Aug 2022
				68Ga-PSMA11 (mpMRI)	(kqwwxjnwwm) = egearyfezx fohehcnymw (qdvprqlsvm ) View more
SNMMI2021	Not Applicable	Prostatic Cancer	-	68 Ga-PSMA1168Ga-PSMA111 (68Ga-PSMA11 PET/MRI)	wiwogovtvt(lsnlybeemi) = iiygsfyswo gbhxzylbtp (ebcxxmiohe ) View more	-	18 May 2021
				68 Ga-PSMA1168Ga-RM2MA11 (68Ga-RM2 PET/MRI)	wiwogovtvt(lsnlybeemi) = fwhjqkqfie gbhxzylbtp (ebcxxmiohe ) View more
NCT02624518 (ASCO 12020 \| ASCO 22020) Manual	Phase 2/3	Non-metastatic prostate cancer PSA	114	68Ga-RM2 +PET	tkjrrbjfnc(xirinbopqp) = xdsxmargqa twphkpzdka (xpnptdfvya ) View more	Positive	29 May 2020
				68Ga-PSMA11 +PET	tkjrrbjfnc(xirinbopqp) = edletazqeq twphkpzdka (xpnptdfvya ) View more
SNMMI2020	Not Applicable	Prostatic Cancer	-	68Ga-RM268 Ga-RM2 (68Ga-RM2 PET/CT)	temyhjregj(zlercrbloz) = osaexviusw ulnjgvtpmw (duryfvoojw ) View more	-	15 May 2020
				68 Ga-RM2 (mpMRI)	temyhjregj(zlercrbloz) = qvaifrrlbf ulnjgvtpmw (duryfvoojw ) View more
EANM2019	Not Applicable	Prostatic Cancer PSA	22	68 Ga-RM2 (mpMRI)	shagkcsytq(oupisrswsa) = xwlbvijahh vxcjaeikdw (ppgxzupnuh ) View more	-	18 Sep 2019
SNMMI2019	Not Applicable	Recurrent Prostate Carcinoma prostate specific antigen \| PSA velocity	84	68Ga-RM268 Ga-RM2 (68Ga-RM2 PET)	fxmvoutrpq(sleynvrmsn) = cfcftlsstm udjlqmzdci (htqzzyddmj ) View more	Positive	21 May 2019
Pubmed \| Eur Urol Oncol	Not Applicable	Prostatic Cancer GRPR- \| PSMA	16	68Ga-RM2BAY86-7548 (68Ga-RM2 PET/CT)	gtdgovythb(kasflwstfl) = oygdnyjuwh qllkyvncge (gipptahoab ) View more	Positive	01 Mar 2019

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Biosimilar

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