Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Lutetium oxodotreotide lu-177
Drug ID BADD_D02568
Description A 177Lu-labeled somatostatin analog peptide, Lutetium Lu 177 dotatate belongs to an emerging form of treatments called Peptide Receptor Radionuclide Therapy (PRRT), which involves targeting tumours with molecules carrying radioactive particles that bind to specific receptors expressed by the tumour. Lutetium Lu 177 dotatate may also be referred to as 177Lu-DOTA-Tyr3-octreotate. Compared to the alternative somatostatin analogue DOTA-Tyr3-octreotide (dotatoc), Lutetium Lu 177 dotatate displays higher uptake of radioactivity in tumors and better residence times [A31696]. In terms of biodistribution, Lutetium Lu 177 dotatate demonstrated a lower whole-body retention, indicating potentially lower risk for bone marrow toxicity [A31696]. The presence of a radioligand allows monitoring of treatment response post therapy and prior to next fraction of the dose delivery which may be clinically beneficial in estimating the intensity of lesion uptakes or deciding the dose for subsequent administrations [A31702]. Lutetium Lu 177 dotatate was approved by the FDA as Lutathera in January 2018 for intravenous injection. It is a first radiopharmaceutical agent to be approved for gastroenteropancreatic neuroendocrine tumors (GEP-NETs) and is indicated for adult patients with somatostatin receptor-positive GEP-NETs [L1191]. Targeting pancreas and other parts of the gastrointestinal tract such as the intestines and colon, neuroendocrine tumors may commonly metastasize to metastasize to the mesentery, peritoneum, and liver [A31697]. Patients with GEP-NETs have limited second-line treatment options after the metastasis of tumors and inadequate therapeutic response from first-line therapies. In a clinical trial involving patients with advanced somatostatin receptor-positive GEP-NET, the treatment of Lutetium Lu 177 dotatate in combination with octreotide resulted in longer progression-free survival compared to patients receiving octreotide alone and there was evidence of an overall survival benefit [A31697].
Indications and Usage Indicated for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults [FDA Label].
Marketing Status approved; investigational
ATC Code V10XX04
DrugBank ID DB13985
KEGG ID D11033
MeSH ID C447941
PubChem ID 76966897
TTD Drug ID D0DQ7V
NDC Product Code 69488-003
UNII AE221IM3BB
Synonyms lutetium Lu 177 dotatate | lutetium (177Lu) oxodotreotide | lutetium oxodotreotide Lu-177 | (177Lu-DOTAOTyr3)octreotate | DOTATATE-177Lu | 177Lu-DOTATATE | (177lutetium-DOTA(O)Tyr3)octreotate | Lu-177 DOTATE | Lutathera
Chemical Information
Molecular Formula C65H87LuN14O19S2
CAS Registry Number 437608-50-9
SMILES CC(C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4= CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)CN6CCN(CCN(CCN(CC6)CC(=O)[O-])CC(=O)[O-]) CC(=O)[O-])C(=O)NC(C(C)O)C(=O)O)O.[Lu+3]
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice.
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal pain07.01.05.002-
Acute hepatic failure09.01.03.001--
Acute myeloid leukaemia16.01.05.001; 01.10.05.001--
Acute respiratory failure14.01.04.004; 22.02.06.001--
Anaemia01.03.02.001-
Aplasia pure red cell10.02.01.003; 01.03.03.001--
Ascites07.07.01.001; 02.05.04.002; 09.01.05.003-
Bone pain15.02.01.001-
Cholecystitis09.03.01.001-
Cholecystitis acute09.03.01.003--
Cholestasis09.01.01.001--
Death08.04.01.001-
Decubitus ulcer23.03.11.006--
Disseminated intravascular coagulation24.01.01.010; 01.01.02.002-
Dyspnoea exertional02.11.05.005; 22.02.01.005--
Eating disorder19.09.01.008; 14.03.01.008--
Electrolyte imbalance14.05.01.002--
Enteritis07.08.03.002-
Extravasation08.01.03.008--
Failure to thrive19.07.05.001; 18.04.01.003; 14.03.02.008--
Flushing24.03.01.002; 23.06.05.003; 08.01.03.025-
Gastrointestinal perforation07.04.04.001--
Generalised oedema14.05.06.007; 08.01.07.004-
Gingival recession07.09.13.012--
Haematemesis24.07.02.011; 07.12.02.002--
Hepatic encephalopathy17.13.01.003; 09.01.03.006--
Hepatic failure09.01.03.002-
Hepatic function abnormal09.01.02.001--
Hepatic necrosis09.01.07.002-
Hepatitis09.01.07.004--
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