Target Information

Target General Information

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Target ID

T26220

Target Name

Somatostatin receptor (SSTR)

Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 2 Target-related Diseases

Melanoma [ICD-11: 2C30]

Stomach cancer [ICD-11: 2B72]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 9 Clinical Trial Drugs

177-Lu-oxodotreotide

Drug Info

Phase 3

Neuroendocrine cancer

[2]

177Lu-DOTA-octreotate

Drug Info

Phase 3

Melanoma

[3]

177Lu-DOTATATE

Drug Info

Phase 2

Hepatitis C virus infection

[4]

Edotreotide

Drug Info

Phase 2

Acromegaly

[5], [6]

FK-962

Drug Info

Phase 2

Alzheimer disease

[7]

Somatoprim

Drug Info

Phase 2

Acromegaly

[8], [9]

177Lu-labelled DOTA-JR11

Drug Info

Phase 1/2

Neuroendocrine cancer

[10]

212Pb-labelled DOTAMTATE

Drug Info

Phase 1

Neuroendocrine cancer

[11]

AlphaMedix

Drug Info

Phase 1

Neuroendocrine cancer

[11]

Discontinued Drug(s)

[+] 3 Discontinued Drugs

BIM-23268

Drug Info

Discontinued in Phase 2

Acromegaly

[12], [13]

FK-960

Drug Info

Discontinued in Phase 2

Cognitive impairment

[14]

SEGLITIDE

Drug Info

Discontinued in Phase 2

Pain

[15], [16]

Mode of Action

[+] 3 Modes of Action

Agonist

[+] 1 Agonist drugs

177-Lu-oxodotreotide

Drug Info

[17]

Modulator

[+] 9 Modulator drugs

177Lu-DOTA-octreotate

Drug Info

[1]

177Lu-DOTATATE

Drug Info

[1]

Edotreotide

Drug Info

[18]

FK-962

Drug Info

[19]

Somatoprim

Drug Info

[20]

BIM-23268

Drug Info

[18]

FK-960

Drug Info

[19]

SEGLITIDE

Drug Info

[24]

Ilatreotide

Drug Info

[25]

Activator

[+] 1 Activator drugs

AlphaMedix

Drug Info

[23]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

References

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REF 1

Peptide receptor radionuclide therapy with 177Lu-DOTATATE for patients with somatostatin receptor-expressing neuroendocrine tumors: the first US phase 2 experience. Pancreas. 2014 May;43(4):518-25.

REF 2

ClinicalTrials.gov (NCT01842165) 177Lutetium-octreotate Treatment Prediction Using Multimodality Imaging in Refractory NETs (LUMEN). U.S. National Institutes of Health.

REF 3

ClinicalTrials.gov (NCT01578239) A Study Comparing Treatment With 177Lu-DOTA0-Tyr3-Octreotate to Octreotide LAR in Patients With Inoperable, Progressive, Somatostatin Receptor Positive Midgut Carcinoid Tumours. U.S. National Institutes of Health.

REF 4

ClinicalTrials.gov (NCT01860742) Randomized Phase III of PRRT Versus Interferon. U.S. National Institutes of Health.

REF 5

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5638).

REF 6

ClinicalTrials.gov (NCT00006370) Radiolabeled SMT-487 (Yttrium Y 90-DOTA-tyr3-octreotide) in Treating Patients With Refractory Small Cell Lung Cancer or Metastatic Breast Cancer. U.S. National Institutes of Health.

REF 7

ClinicalTrials.gov (NCT00087724) A Randomized Study to Evaluate FK962 in Subjects With Mild to Moderate Alzheimer's Disease. U.S. National Institutes of Health.

REF 8

REF 9

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016053)

REF 10

ClinicalTrials.gov (NCT02592707) Study to Evaluate the Safety and Preliminary Efficacy of 177Lu-OPS201 in NETs. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT03466216) Phase 1 Study of AlphaMedix in Adult Subjects With SSTR (+) NET. U.S. National Institutes of Health.

REF 12

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016700)

REF 14

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008887)

REF 15

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000642)

REF 17

Lutetium-labelled peptides for therapy of neuroendocrine tumours. Eur J Nucl Med Mol Imaging. 2012 Feb;39 Suppl 1(Suppl 1):S103-12.

REF 18

Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

REF 19

FK960, a novel potential anti-dementia drug, enhances high K(+)-evoked release of somatostatin from rat hippocampal slices. Brain Res. 2001 Feb 16;892(1):111-7.

REF 20

DG3173 (somatoprim), a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue, effectively reduces GH secretion in human GH-secreting pituitary adenomas even in Octreotide non-responsive tumours.Eur J Endocrinol.2012 Feb;166(2):223-34.

REF 21

Multimodal Imaging of 2-Cycle PRRT with 177 Lu-DOTA-JR11 and 177 Lu-DOTATOC in an Orthotopic Neuroendocrine Xenograft Tumor Mouse Model. J Nucl Med. 2021 Mar;62(3):393-398.

REF 22

Radiopharmaceutical therapy in cancer: clinical advances and challenges. Nat Rev Drug Discov. 2020 Sep;19(9):589-608.

REF 23

Clinical pipeline report, company report or official report of Orano Med.

REF 24

Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria.. Br J Pharmacol. 1993 August; 109(4): 898-899.

REF 25

Inhibitory effect of intraduodenal administration of somatostatin analogue SDZ CO 611 on rat pancreatic exocrine secretion. Pancreas. 1993 Jul;8(4):471-5.

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