rhenium-186 hedp profile

Rhenium-186 HEDP, also known as [186Re]HEDP, is a radiopharmaceutical used in nuclear medicine for the treatment of bone pain associated with metastatic bone cancer. It is a complex formed between the radioactive isotope rhenium-186 and the chelating agent hydroxyethylidene diphosphonate (HEDP). The compound is synthesized by reacting rhenium-186 with HEDP in a weakly acidic solution. The resulting complex has a high affinity for bone tissue, where it localizes and emits beta radiation, which effectively alleviates bone pain by targeting and destroying cancerous cells. The use of rhenium-186 HEDP for bone pain palliation is based on its ability to deliver radiation directly to the tumor site, reducing the need for high doses of systemic analgesics. The compound's high bone targeting and low systemic toxicity make it a safe and effective treatment option for bone pain management in cancer patients. Ongoing research focuses on optimizing the synthesis process and further exploring the therapeutic potential of this compound for various bone-related conditions, including bone infections and osteoporosis.'

rhenium-186 HEDP: used as a complement to analgesic therapy in patients with painful disseminated bone metastases [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	121982
MeSH ID	M0266290

Synonym
rhenium-186 hedp
186re hedp
rhenium-hydroxyethylidene diphosphonate
rhenium-188 hydroxyethylidene diphosphonate
(186re)-hydroxyethylidene diphosphonate
140709-07-5
phosphonic acid, (1-hydroxyethylidene)bis-, rhenium-186re salt
unii-dv7w6w681s
(1-hydroxyethylidene)bisphosphonic acid rhenium-186re salt
DTXSID80161466
Q27276621
(1-hydroxy-1-phosphonooxyethyl) dihydrogen phosphate;rhenium-186

Excerpt	Reference	Relevance
" No major adverse effects were observed."	( Evaluation of toxicity and efficacy of 186Re-hydroxyethylidene diphosphonate in patients with painful bone metastases of prostate or breast cancer. Carpentier, P; Caty, A; Depreux, P; Kolesnikov-Gauthier, H; Sulman, C; Vennin, P, 2000)	0.31
"186Re-HEDP provides safe symptomatic relief of pain in prostate cancer patients."	( Evaluation of toxicity and efficacy of 186Re-hydroxyethylidene diphosphonate in patients with painful bone metastases of prostate or breast cancer. Carpentier, P; Caty, A; Depreux, P; Kolesnikov-Gauthier, H; Sulman, C; Vennin, P, 2000)	0.31
"Retreatments with (186)Re-HEDP under zoledronic acid provide continuing effectiveness in metastatic bone pain and are safe enough, if an acceptable baseline hematologic status exists."	( Management of metastatic bone pain with repeated doses of rhenium 186-HEDP in patients under therapy with zoledronic acid: a safe and additively effective practice. Baziotis, N; Limouris, GS; Zafeirakis, A; Zissimopoulos, A, 2009)	0.35

Excerpt	Reference	Relevance
" In both dose levels, cabazitaxel (4 cycles of cabazitaxel 25 mg/m + 2 cycles of cabazitaxel 20 mg/m in level 1, and 6 cycles of cabazitaxel 25 mg/m in level 2) were combined with 2 cycles of Re-HEDP 40 MBq/kg (1."	( A Phase 1 Trial of Cabazitaxel Combined With 188Re-Hydroxyethylidene Diphosphonate in Patients With Metastatic Castration-Resistant Prostate Cancer Who Progressed on or After a Docetaxel-Containing Treatment: The ReCab Trial. Bloemendal, HJ; Bouman-Wammes, EW; de Klerk, JMH; van den Eertwegh, AJM; van Dodewaard-de Jong, JM; Verheul, HMW, 2017)	0.46

Excerpt	Relevance	Reference
" This paper reports the results of dosage escalation studies with 186Re-HEDP as a bone-seeking radiopharmaceutical in patients with bone metastases originating from breast or prostate cancer with regard to toxicity, pharmacokinetics and bone marrow dosimetry and the palliating effect on bone pain."	( Treatment of metastatic bone pain using the bone seeking radiopharmaceutical Re-186-HEDP. Blijham, GH; De Klerk, JM; Han, SH; Hoekstra, A; Quirijnen, JM; Van Dijk, A; Van Het Schip, AD; Van Rijk, PP; Zonnenberg, BA, )	0.13
" No clear dose-response relationship was found."	( 186Re-etidronate in breast cancer patients with metastatic bone pain. Blijham, GH; de Klerk, JM; Han, SH; Quirijnen, JM; van Dijk, A; van het Schip, AD; van Rijk, PP; Zonneberg, BA, 1999)	0.3
" Of the six patients treated at the highest dosage schedules (three at 1510 MBq/m2 and three at 1665 MBq/m2), three showed a posttherapy decline in prostate-specific antigen of 50% or more."	( Rhenium-186-labeled hydroxyethylidene diphosphonate dosimetry and dosing guidelines for the palliation of skeletal metastases from androgen-independent prostate cancer. Curley, T; Daghighian, F; Goldsmith, SJ; Graham, MC; Larson, SM; Liu, GB; Scher, HI; Yeh, SD, 1999)	0.3
" However, by this new scintigraphic quantification method, bone uptake and soft-tissue retention can be calculated separately, thus providing more detailed kinetic data and potentially improving the dosimetry of these radiopharmaceuticals in, for example, assessment of radiation dosage to bone and bone marrow."	( Skeletal uptake and soft-tissue retention of 186Re-HEDP and 153Sm-EDTMP in patients with metastatic bone disease. Brenner, W; Henze, E; Kampen, AM; Kampen, WU, 2001)	0.31
" The dosage of opiates was decreased in 77% of the patients and could be discontinued in 4 of them."	( Palliative treatment of painful disseminated bone metastases with 186Rhenium-HEDP in patients with lung cancer. Anagnostopoulou, US; Datseris, EI; Leondi, AH; Leontopoulou, SA; Papadaki, EK; Rapti, AS; Souvatzoglou, MA; Zerva, CJ, 2004)	0.32
"A dose escalation schedule was designed consisting of four dose levels with a standard dosage of docetaxel (75 mg/m(2) 3-weekly)."	( A phase I study of combined docetaxel and repeated high activity 186Re-HEDP in castration-resistant prostate cancer (CRPC) metastatic to bone (the TAXIUM trial). Bloemendal, HJ; de Haas, MJ; de Klerk, JM; O'Sullivan, JM; van Bezooijen, BP; van Dodewaard-de Jong, JM; Wilson, RH, 2011)	0.37
" This study shows the importance of patient stratification to establish absorbed dose-response correlations and indicates the potential to individualise treatment of bone metastases with radiopharmaceuticals according to patient-specific imaging and dosimetry."	( Phase I/II trials of Chittenden, SJ; Dearnaley, DP; Denis-Bacelar, AM; Divoli, A; Du, Y; Flux, GD; Johnson, B; McCready, VR; O'Sullivan, JM, 2017)	0.46

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	11 (16.42)	18.2507
2000's	37 (55.22)	29.6817
2010's	19 (28.36)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	32 (42.67%)	5.53%
Reviews	7 (9.33%)	6.00%
Case Studies	3 (4.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	33 (44.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces.	14.23	67	27	1,1-bis(phosphonic acid)	antineoplastic agent; bone density conservation agent; chelator
pamidronate [no description available]	3.41	1	1	phosphonoacetic acid
prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.	3.53	1	1	11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug
deoxycytidine [no description available]	2.04	1	0	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
durapatite Durapatite: The mineral component of bones and teeth; it has been used therapeutically as a prosthetic aid and in the prevention and treatment of osteoporosis.. hydroxylapatite : A phosphate mineral with the formula Ca5(PO4)3(OH).	2.04	1	0
(ethylenedinitrilo)-tetramethylenephosphonic acid (ethylenedinitrilo)-tetramethylenephosphonic acid: structure; RN given refers to parent cpd	2.15	1	0
rhenium Rhenium: A metal, atomic number 75, atomic weight 186.207, symbol Re.	11.39	38	16	manganese group element atom
samarium Samarium: An element of the rare earth family of metals. It has the atomic symbol Sm, atomic number 62, and atomic weight 150.36. The oxide is used in the control rods of some nuclear reactors.	2	1	0	f-block element atom; lanthanoid atom
scandium Scandium: An element of the rare earth family of metals. It has the atomic symbol Sc, atomic number 21, and atomic weight 45.	2.15	1	0	d-block element atom; rare earth metal atom; scandium group element atom
hydroxymethanediphosphonic acid hydroxymethanediphosphonic acid: RN given refers to parent cpd	2	1	0	1,1-bis(phosphonic acid)
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	2.04	1	0	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.	2.05	1	0	1,1-bis(phosphonic acid); imidazoles	bone density conservation agent
technetium tc 99m hydroxymethylene diphosphonate technetium Tc 99m hydroxymethylene diphosphonate: bone-seeking radiopharmaceutical	3.81	3	0
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	5.34	4	3	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
organophosphonates hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.	2	1	0	divalent inorganic anion; phosphite ion
melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.	2.02	1	0	L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound	alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent
strontium Strontium: An element of the alkaline earth family of metals. It has the atomic symbol Sr, atomic number 38, and atomic weight 87.62.	7.53	6	1	alkaline earth metal atom
strontium radioisotopes Strontium Radioisotopes: Unstable isotopes of strontium that decay or disintegrate spontaneously emitting radiation. Sr 80-83, 85, and 89-95 are radioactive strontium isotopes.	7.08	5	2
radium Radium: A radioactive element of the alkaline earth series of metals. It has the atomic symbol Ra and atomic number 88. Radium is the product of the disintegration of URANIUM and is present in pitchblende and all ores containing uranium. It is used clinically as a source of beta and gamma-rays in radiotherapy, particularly BRACHYTHERAPY.	4.14	1	0	alkaline earth metal atom
cabazitaxel cabazitaxel: an antineoplastic agent; structure in first source. cabazitaxel : A tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly.	3.94	2	1	tetracyclic diterpenoid	antineoplastic agent; microtubule-stabilising agent
technetium tc 99m medronate Technetium Tc 99m Medronate: A gamma-emitting radionuclide imaging agent used primarily in skeletal scintigraphy. Because of its absorption by a variety of tumors, it is useful for the detection of neoplasms.	4.04	4	0

Condition	Relationship Strength	Studies	Trials
Bone Cancer [description not available]	13.67	58	23
Androgen-Independent Prostatic Cancer [description not available]	6.84	4	2
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	13.67	58	23
Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.	6.84	4	2
Ache [description not available]	10.34	30	10
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	10.34	30	10
Cancer of Prostate [description not available]	10.1	32	16
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	10.1	32	16
Cancer-Associated Pain [description not available]	5.75	2	1
Cancer Pain Pain that may be caused by or related to cellular, tissue, and systemic changes that occur during NEOPLASM growth, tissue invasion, and METASTASIS.	5.75	2	1
Breast Cancer [description not available]	8.5	16	10
Breast Neoplasms Tumors or cancer of the human BREAST.	8.5	16	10
Disease Exacerbation [description not available]	5.95	3	3
Metastase [description not available]	11.63	7	3
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	6.63	7	3
Benign Neoplasms [description not available]	4.75	2	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	4.75	2	1
Pain, Intractable Persistent pain that is refractory to some or all forms of treatment.	6.14	4	3
Leukocytopenia [description not available]	2.93	1	0
Thrombopenia [description not available]	4.71	2	1
Leukopenia A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000).	2.93	1	0
Thrombocytopenia A subnormal level of BLOOD PLATELETS.	4.71	2	1
Cancer of Lung [description not available]	4.09	3	1
Lung Neoplasms Tumors or cancer of the LUNG.	4.09	3	1
Injuries, Radiation [description not available]	2.93	1	0
Carcinoma, Anaplastic [description not available]	3.4	1	1
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	3.4	1	1
Kahler Disease [description not available]	2.02	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	2.02	1	0
Osteogenic Sarcoma [description not available]	3.41	1	1
Osteosarcoma A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)	3.41	1	1
Charcot's Joint [description not available]	3.42	1	1
Joint Pain [description not available]	3.42	1	1
Autosomal Hemophilia A [description not available]	3.42	1	1
Hemarthrosis Bleeding into the joints. It may arise from trauma or spontaneously in patients with hemophilia.	3.42	1	1
Arthropathy, Neurogenic Chronic progressive degeneration of the stress-bearing portion of a joint, with bizarre hypertrophic changes at the periphery. It is probably a complication of a variety of neurologic disorders, particularly TABES DORSALIS, involving loss of sensation, which leads to relaxation of supporting structures and chronic instability of the joint. (Dorland, 27th ed)	3.42	1	1
Hemophilia A The classic hemophilia resulting from a deficiency of factor VIII. It is an inherited disorder of blood coagulation characterized by a permanent tendency to hemorrhage.	3.42	1	1
Arthralgia Pain in the joint.	3.42	1	1
Neoplasms, Bone Marrow [description not available]	3.38	1	1
Bone Marrow Neoplasms Neoplasms located in the bone marrow. They are differentiated from neoplasms composed of bone marrow cells, such as MULTIPLE MYELOMA. Most bone marrow neoplasms are metastatic.	3.38	1	1
Soft Tissue Neoplasms Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.	2	1	0
Cancer of Nasopharynx [description not available]	2	1	0
Cancer of Rectum [description not available]	2	1	0
Nasopharyngeal Neoplasms Tumors or cancer of the NASOPHARYNX.	2	1	0
Rectal Neoplasms Tumors or cancer of the RECTUM.	2	1	0
Adenocarcinoma, Basal Cell [description not available]	3.39	1	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	3.39	1	1
Rheumatoid Arthritis [description not available]	3.39	1	1
Arthritis, Rheumatoid A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.	3.39	1	1

rhenium-186 hedp

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Synonyms (12)

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Research

Studies (67)

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Research Demand Index: 9.89

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