Syed Mohammed Nuruddin

• Staniszewska, Magdalena; Hübner, Ralph; Locatelli, Camilla; Howard, Douglas; Forni, Matilde & Man, Francis [Vis alle 13 forfattere av denne artikkelen] (2026). Ensuring enantiomeric consistency in FAPI radiopharmaceuticals: comparative analysis of (S)- and (S/R)-FAPI-46/-74 confirms pharmacological equivalence. EJNMMI Radiopharmacy and Chemistry. 11(1). doi: 10.1186/s41181-026-00432-4. Fulltekst i vitenarkiv Vis sammendrag

  Background Enantiomeric composition may impact binding and potentially performance of a drug product but is not routinely tested and minimum acceptance criteria are not always established. Some batches of the precursors FAPI-46 and FAPI-74 used clinically contain a mixture of (S)- and (R)-enantiomers. This study investigates the in vitro pharmacodynamic characteristics of different enantiomeric compositions of FAP-targeting radioligands FAPI-46 and FAPI-74 and in vivo pharmacokinetics of FAPI-46 in naïve mice. Results (S)-, (R)-, and (S/R)-enantiomers of radiolabeled FAPI-46 and FAPI-74 were evaluated for stability in human serum, binding affinity, internalization, retention, and selectivity using HT1080-hFAP cells and HEK293-hCD26 cells. All enantiomeric compositions showed high stability in human serum with minimal serum protein adhesion. (S)- and (S/R)-enantiomers exhibited comparable binding, internalization, and retention characteristics. High selectivity for FAP over CD26/DPP4 was maintained. (R)-enantiomers showed no specific binding to FAP. Additionally, the same enantiomers of 68Ga-labeled FAPI-46 were evaluated by dynamic positron emission tomography (PET) imaging (0–60 min post-injection) and ex vivo organ biodistribution in naïve BALB/c mice (10, 30, and 60 min, or 4 h post-injection) to compare their pharmacokinetic profiles. PET imaging revealed nearly identical time-activity curves for the enantiomers of [68Ga] Ga-FAPI-46, indicating similar whole-body distribution within 1 h post-injection, with rapid renal clearance and minimal muscle uptake. Ex vivo organ biodistribution confirmed comparable pharmacokinetic profiles between enantiomers, with no significant differences in tissue distribution. Conclusion These findings provide important validation that current clinical (S/R)-mixtures of FAPI-46/-74 exhibit pharmacokinetic and pharmacodynamic behavior comparable to pure (S)-enantiomers, supporting regulatory confidence and cross-trial reproducibility in the global FAPI-46/-74 imaging landscape.

• Lien, Vegard Torp; Hauge, Emily; Nuruddin, Syed Mohammad; Klaveness, Jo & Olberg, Dag Erlend (2023). Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer. Journal of labelled compounds & radiopharmaceuticals. ISSN 0362-4803. 66(14), s. 452–460. doi: 10.1002/jlcr.4066. Fulltekst i vitenarkiv
• Stokke, Caroline; Nørgaard, Jakob Nordberg; Phillips, Hilde Feiring; Sherwani, Alexander Gul; Nuruddin, Syed Mohammad & Connelly, James Pattrick [Vis alle 8 forfattere av denne artikkelen] (2022). Comparison of [18F]fluciclovine and [18F]FDG PET/CT in Newly Diagnosed Multiple Myeloma Patients. Molecular Imaging and Biology. ISSN 1536-1632. 24(5), s. 842–851. doi: 10.1007/s11307-022-01734-0. Fulltekst i vitenarkiv Vis sammendrag

  Abstract Purpose [ 18 F]FDG PET/CT in multiple myeloma (MM) is currently the best technology to demonstrate patchy and extramedullary disease. However, [ 18 F]FDG PET has some limitations, and imaging with alternative tracers should be explored. In this study, we aimed to evaluate the performance of [ 18 F]fluciclovine PET compared to [ 18 F]FDG PET in newly diagnosed MM patients. Procedures Thirteen newly diagnosed transplant eligible MM patients were imaged both with [ 18 F]FDG PET/CT and [ 18 F]fluciclovine PET/CT within 1 week in a prospective study. The subjects were visually assessed positive or negative for disease. The number of lesions and the SUV max of selected lesions were measured for both tracers. Furthermore, tracer uptake ratios were obtained by dividing lesion SUV max by blood or bone marrow SUV max . Between-group differences and correlations were assessed with paired t -tests and Pearson tests. Bone marrow SUVs were compared to bone marrow plasma cell percentage in biopsy samples. Results Nine subjects were assessed positively by [ 18 F]FDG PET (69%) and 12 positives by [ 18 F]fluciclovine PET (92%). All positive subjects had [ 18 F]fluciclovine scans that were qualitatively scored as easier to interpret visually than the [ 18 F]FDG scans. The number of lesions was also higher; seven of nine subjects with distinct hot spots on [ 18 F]fluciclovine PET had fewer or no visible lesions on [ 18 F]FDG PET. The mean lesion SUV max values were 8.2 and 3.8 for [ 18 F]fluciclovine and [ 18 F]FDG, respectively. The mean tumour to blood values were 6.4 and 2.0 for [ 18 F]fluciclovine and [ 18 F]FDG, and the mean ratios between tumour and bone marrow were 2.1 and 1.5 for [ 18 F]fluciclovine and [ 18 F]FDG. The lesion SUV max and ratios were significantly higher for [ 18 F]fluciclovine (all p  < 0.01). Local [ 18 F]fluciclovine SUV max or SUV mean values in os ilium and the percentage of plasma cells in bone marrow biopsies were linearly correlated ( p  = 0.048). There were no significant correlations between [ 18 F]FDG SUVs and plasma cells ( p  = 0.82). Conclusions Based on this pilot study, [ 18 F]fluciclovine is a promising tracer for MM. The visual and semi-quantitative evaluations indicate that [ 18 F]fluciclovine PET/CT can out-perform [ 18 F]FDG PET/CT at diagnosis.

• Lien, Vegard Torp; Celen, Sofie; Nuruddin, Syed; Attili, Bala; Doumont, Gilles & Simaeys, Gaetan Van [Vis alle 9 forfattere av denne artikkelen] (2021). Preclinical evaluation of [18F]cabozantinib as a PET imaging agent in a prostate cancer mouse model. Nuclear Medicine and Biology. ISSN 0969-8051. 93, s. 74–80. doi: 10.1016/j.nucmedbio.2020.12.002. Fulltekst i vitenarkiv
• Bekker, Roberto Bartholomeus Wilhelmus; Fjellaksel, Richard; Hjornevik, Trine; Nuruddin, Syed; Rafique, Waqas & Hansen, Jørn H [Vis alle 9 forfattere av denne artikkelen] (2020). Discovery of a lead brain-penetrating gonadotropin-releasing hormone receptor antagonist with saturable binding in brain. ChemMedChem. ISSN 1860-7179. 15(17), s. 1624–1628. doi: 10.1002/cmdc.202000256. Fulltekst i vitenarkiv Vis sammendrag

  We report the synthesis, radiosynthesis and biological characterisation of two gonadotropin‐releasing hormone receptor (GnRH−R) antagonists with nanomolar binding affinity. A small library of GnRH−R antagonists was synthesised in 20–67 % overall yield with the aim of identifying a high‐affinity antagonist capable of crossing the blood–brain barrier. Binding affinity to rat GnRH−R was determined by autoradiography in competitive‐binding studies against [¹²⁵l]buserelin, and inhibition constants were calculated by using the Cheng–Prusoff equation. The radioligands were obtained in 46–79 % radiochemical yield and >95 % purity and with a molar activity of 19–38 MBq/nmol by direct nucleophilic radiofluorination. Positron emission tomography imaging in rat under baseline conditions in comparison to pretreatment with a receptor‐saturating dose of GnRH antagonist revealed saturable uptake (0.1 %ID/mL) into the brain.

• Tungen, Jørn Eivind; Aursnes, Marius; Ramon, Sesquile; Colas, Romain A.; Serhan, Charles Nicholas & Olberg, Dag Erlend [Vis alle 9 forfattere av denne artikkelen] (2018). Synthesis of Protectin D1 Analogs: Novel Pro-resolution and Radiotracer Agents. Organic and biomolecular chemistry. ISSN 1477-0520. 16, s. 6818–6823. doi: 10.1039/c8ob01232f. Fulltekst i vitenarkiv
• Nuruddin, Syed; Syverstad, Gry-Helen Enger; Lillehaug, Sveinung; Leergaard, Trygve Brauns; Nilsson, Lars & Ropstad, Erik [Vis alle 9 forfattere av denne artikkelen] (2014). Elevated mRNA-Levels of Gonadotropin-Releasing Hormone and Its Receptor in Plaque-Bearing Alzheimer's Disease Transgenic Mice. PLOS ONE. 9(8). doi: 10.1371/journal.pone.0103607. Fulltekst i vitenarkiv
• Nuruddin, Syed; Bruchhage, Muriel; Ropstad, Erik; Krogenæs, Anette; Evans, Neil P. & Robinson, Jane E. [Vis alle 10 forfattere av denne artikkelen] (2013). Effects of peripubertal gonadotropin-releasing hormone agonist on brain development in sheep-A magnetic resonance imaging study. Psychoneuroendocrinology. ISSN 0306-4530. 38(10), s. 1994–2002. doi: 10.1016/j.psyneuen.2013.03.009. Fulltekst i vitenarkiv
• Nuruddin, Syed; Krogenæs, Anette; Brynildsrud, Ola Brønstad; Verhaegen, Steven; Evans, Neil P. & Robinson, Jane E. [Vis alle 8 forfattere av denne artikkelen] (2013). Peri-pubertal gonadotropin-releasing hormone agonist treatment affects sex biased gene expression of amygdala in sheep. Psychoneuroendocrinology. ISSN 0306-4530. 38, s. 3115–3127. doi: 10.1016/j.psyneuen.2013.09.011. Fulltekst i vitenarkiv
• Nuruddin, Syed; Wojniusz, Slawomir; Ropstad, Erik; Krogenæs, Anette; Evans, Neil P. & Robinson, Jane E. [Vis alle 9 forfattere av denne artikkelen] (2013). Peri-pubertal gonadotropin-releasing hormone analog treatment affects hippocampus gene expression without changing spatial orientation in young sheep. Behavioural Brain Research. ISSN 0166-4328. 242, s. 9–16. doi: 10.1016/j.bbr.2012.12.027. Fulltekst i vitenarkiv

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• Reinertsen, Amalie Føreid; Hansen, Trond Vidar; Nuruddin, Syed Mohammad & Serhan, Charles N (2024). Stereoselective Synthesis and Biological Evaluations of Pro-resolution and Radiotracer Agents. Fulltekst i vitenarkiv
• Lien, Vegard Torp; Hauge, Emily; Nuruddin, Syed; Klaveness, Jo & Olberg, Dag Erlend (2019). Synthesis and preclinical evaluation of a selective c-Met PET tracer. Fulltekst i vitenarkiv
• Nuruddin, Syed; Bruchhage, Muriel; Ropstad, Erik; Krogenæs, Anette; Evans, Neil P. & Robinson, J [Vis alle 10 forfattere av denne artikkelen] (2014). Corrigendum to Effects of peripubertal gonadotropin-releasing hormone agonist on brain development in sheep - A magnetic resonance imaging study [Psychoneuroendocrinology, 38(10), (2013), 1994-2002]. Psychoneuroendocrinology. ISSN 0306-4530. 40(1), s. 286–286. doi: 10.1016/j.psyneuen.2013.10.016. Fulltekst i vitenarkiv
• Syverstad, Gry-Helen Enger; Nuruddin, Syed; Lillehaug, Sveinung; Leergaard, Trygve B.; Haraldsen, Ira Hebold & Torp, Reidun (2013). Targeting gonadotroping-releasing hormone in Alzheimer’s disease. Fulltekst i vitenarkiv

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