PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
23788266-0	2013	Development and validation of an RP-HPLC method for the quantitation of Orteronel (TAK-700), a CYP17A1 enzyme inhibitor, in rat plasma and its application to a pharmacokinetic study.	orteronel	72-81	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	95-102
23788266-0	2013	Development and validation of an RP-HPLC method for the quantitation of Orteronel (TAK-700), a CYP17A1 enzyme inhibitor, in rat plasma and its application to a pharmacokinetic study.	orteronel	83-90	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	95-102
32223238-0	2020	Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.	orteronel	50-59	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	85-105
34824002-0	2022	A Phase II Study Evaluating Orteronel, an Inhibitor of Androgen Biosynthesis, in Patients With Androgen Receptor (AR)-Expressing Metastatic Breast Cancer (MBC).	orteronel	28-37	androgen receptor	Homo sapiens	95-112
34824002-0	2022	A Phase II Study Evaluating Orteronel, an Inhibitor of Androgen Biosynthesis, in Patients With Androgen Receptor (AR)-Expressing Metastatic Breast Cancer (MBC).	orteronel	28-37	androgen receptor	Homo sapiens	114-116
34824002-6	2022	Orteronel was administered at 300 mg BID; response rate was the primary endpoint.	orteronel	0-9	BH3 interacting domain death agonist	Homo sapiens	37-40
33004739-2	2020	Many randomized controlled trials (RCTs) showed promising results that men with metastatic castration-resistant PCa (mCRPC) might benefit from treatment with CYP17 inhibitors such as abiraterone acetate and orteronel.	orteronel	207-216	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	158-163
28373265-7	2017	However, (S)-orteronel and (R)-orteronel bind to distinct CYP17A1 conformations that differ in a region implicated in ligand entry/exit and the presence of a peripheral ligand.	orteronel	9-22	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	58-65
31017696-13	2019	Furthermore, Prog-induced AR translocation was not affected by treatment with TAK700 or abiraterone, while it was effectively blocked by the AR antagonist enzalutamide, further demonstrating the direct AR activation by Prog.	orteronel	78-84	androgen receptor	Homo sapiens	26-28
28463227-5	2017	Here, we have demonstrated that CYP17 inhibitors, with the exception of orteronel, can function as competitive AR antagonists.	orteronel	72-81	androgen receptor	Homo sapiens	111-113
25701170-0	2015	Orteronel plus prednisone in patients with chemotherapy-naive metastatic castration-resistant prostate cancer (ELM-PC 4): a double-blind, multicentre, phase 3, randomised, placebo-controlled trial.	orteronel	0-9	proprotein convertase subtilisin/kexin type 4	Homo sapiens	115-119
27826831-0	2017	Phase 1b study of orteronel in postmenopausal women with hormone-receptor positive (HR+) metastatic breast cancer.	orteronel	18-27	nuclear receptor subfamily 4 group A member 1	Homo sapiens	57-73
27826831-3	2017	Thus, we conducted a phase 1b study of orteronel in postmenopausal women with hormone-receptor positive (HR+) metastatic breast cancer.	orteronel	39-48	nuclear receptor subfamily 4 group A member 1	Homo sapiens	78-94
27826831-15	2017	Conclusions Orteronel 400 mg BID is well tolerated in postmenopausal women, and significantly suppresses serum estrogens and testosterone.	orteronel	12-21	BH3 interacting domain death agonist	Homo sapiens	29-32
26418412-6	2016	The uptake study using rat kidney slices suggested that the transport of orteronel from the blood circulation to the kidney was mediated by a digoxin sensitive transport system represented by Oatp4c1 and non-saturable components.	orteronel	73-82	solute carrier organic anion transporter family, member 4C1	Rattus norvegicus	192-199
26382777-0	2015	Re: Phase III, Randomized, Double-Blind, Multicenter Trial Comparing Orteronel (TAK-700) plus Prednisone with Placebo plus Prednisone in Patients with Metastatic Castration-Resistant Prostate Cancer that has Progressed during or after Docetaxel-Based Therapy: ELM-PC 5.	orteronel	69-78	proprotein convertase subtilisin/kexin type 5	Homo sapiens	264-268
26971992-1	2016	Abiraterone acetate and orteronel are two CYP-17 inhibitors that have been studied in prostate cancer.	orteronel	24-33	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	42-48
25297456-0	2016	Preclinical assessment of Orteronel( ), a CYP17A1 enzyme inhibitor in rats.	orteronel	26-35	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	42-49
25297456-1	2016	Orteronel (TAK-700) is a novel and selective inhibitor of CYP17A1, which is expressed in testicular, adrenal and prostate tumor tissues.	orteronel	0-9	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	58-65
25297456-1	2016	Orteronel (TAK-700) is a novel and selective inhibitor of CYP17A1, which is expressed in testicular, adrenal and prostate tumor tissues.	orteronel	11-18	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	58-65
25560485-13	2015	Furthermore, the most recently identified CYP17A1 inhibitors Orteronel, Galeterone, VT-464, and CFG920 will also be explored.	orteronel	61-70	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	42-49
23856460-0	2013	Effect of an investigational CYP17A1 inhibitor, orteronel (TAK-700), on estrogen- and corticoid-synthesis pathways in hypophysectomized female rats and on the serum estradiol levels in female cynomolgus monkeys.	orteronel	48-57	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	29-36
25537627-13	2015	Dose-dependent increase in plasma orteronel concentrations was indicated over the 200-400 mg BID dose range.	orteronel	34-43	BH3 interacting domain death agonist	Homo sapiens	93-96
25537627-17	2015	CONCLUSIONS: Orteronel at doses up to 400 mg BID was tolerable in Japanese CRPC patients.	orteronel	13-22	BH3 interacting domain death agonist	Homo sapiens	45-48
24965748-0	2014	Phase II study of single-agent orteronel (TAK-700) in patients with nonmetastatic castration-resistant prostate cancer and rising prostate-specific antigen.	orteronel	31-40	kallikrein related peptidase 3	Homo sapiens	130-155
24965748-0	2014	Phase II study of single-agent orteronel (TAK-700) in patients with nonmetastatic castration-resistant prostate cancer and rising prostate-specific antigen.	orteronel	42-49	kallikrein related peptidase 3	Homo sapiens	130-155
24965748-3	2014	EXPERIMENTAL DESIGN: Patients with nmCRPC and rising prostate-specific antigen (PSA) received orteronel 300 mg twice daily until PSA progression, metastases, or unacceptable toxicity.	orteronel	94-103	kallikrein related peptidase 3	Homo sapiens	53-84
24965748-3	2014	EXPERIMENTAL DESIGN: Patients with nmCRPC and rising prostate-specific antigen (PSA) received orteronel 300 mg twice daily until PSA progression, metastases, or unacceptable toxicity.	orteronel	94-103	kallikrein related peptidase 3	Homo sapiens	80-83
24965748-13	2014	CONCLUSIONS: Single-agent orteronel produced marked and durable declines in PSA in patients with nmCRPC.	orteronel	26-35	kallikrein related peptidase 3	Homo sapiens	76-79
23856460-11	2013	In summary, orteronel can suppress serum estradiol concentrations in hypophysectomized female rats and monkeys through selective inhibition of CYP17A1 activity, suggesting that orteronel might be effective for hormone-dependent breast cancers and estrogen-dependent diseases.	orteronel	177-186	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	143-150
25264242-3	2014	Human liver microsomal studies indicated that orteronel weakly inhibits CYP1A2, 2C8, 2C9 and 2C19, with IC50 values of 17.8, 27.7, 30.8 and 38.8 microm, respectively, whereas orteronel does not inhibit CYP2B6, 2D6 or 3A4/5 (IC50  > 100 microm).	orteronel	46-55	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	72-78
25264242-3	2014	Human liver microsomal studies indicated that orteronel weakly inhibits CYP1A2, 2C8, 2C9 and 2C19, with IC50 values of 17.8, 27.7, 30.8 and 38.8 microm, respectively, whereas orteronel does not inhibit CYP2B6, 2D6 or 3A4/5 (IC50  > 100 microm).	orteronel	46-55	cytochrome P450 family 2 subfamily B member 6	Homo sapiens	202-208
25264242-6	2014	Therefore, a physiologically based pharmacokinetic (PBPK) model was developed to assess the potential for drug-drug interactions (DDIs) between orteronel and theophylline, repaglinide, (S)-warfarin and omeprazole, which are sensitive substrates of CYP1A2, 2C8, 2C9 and 2C19, respectively.	orteronel	144-153	cytochrome P450 family 1 subfamily A member 2	Homo sapiens	248-254
24799061-2	2014	Orteronel inhibits the 17,20 lyase activity of the enzyme CYP17A1, which is important for androgen synthesis in the testes, adrenal glands and prostate cancer cells.	orteronel	0-9	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	58-65
24799061-4	2014	Early reports of clinical studies demonstrate that orteronel treatment leads to reduced prostate-specific antigen levels, a marker of prostate cancer tumor burden, and more complete suppression of androgen synthesis than conventional androgen deprivation therapies that act in the testes alone.	orteronel	51-60	kallikrein related peptidase 3	Homo sapiens	88-113
24418642-11	2014	CONCLUSIONS: 17,20-Lyase inhibition by orteronel was tolerable and results in declines in PSA and testosterone, with evidence of radiographic responses.	orteronel	39-48	kallikrein related peptidase 3	Homo sapiens	90-93
24844235-3	2014	Based on these observations, potent agents targeting the AR axis were developed: 1) inhibitors of CYP17 (a key enzyme in the production of androgens), such as abiraterone and orteronel; 2) AR antagonists that bind to AR and impair AR activation, such as enzalutamide and ARN-509.	orteronel	175-184	androgen receptor	Homo sapiens	57-59
23856460-1	2013	Orteronel (TAK-700) is an investigational, non-steroidal inhibitor of CYP17A1 with preferential inhibition of 17,20-lyase in NCI-H295 cells.	orteronel	0-9	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	70-77
23856460-1	2013	Orteronel (TAK-700) is an investigational, non-steroidal inhibitor of CYP17A1 with preferential inhibition of 17,20-lyase in NCI-H295 cells.	orteronel	11-18	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	70-77
23856460-8	2013	Orteronel at 15mg/kg/day (7.5mg/kg/treatment, twice daily [bid]) continued to suppress the estradiol surge prior to the start of luteal phase for 1.5-times the average duration of three consecutive, pre-treatment menstrual cycles, while serum progesterone was maintained at levels almost equal to those in the luteal phase although a certain portion of this increased level of progesterone could be of adrenal-origin.	orteronel	0-9	BH3 interacting domain death agonist	Rattus norvegicus	59-62
23856460-11	2013	In summary, orteronel can suppress serum estradiol concentrations in hypophysectomized female rats and monkeys through selective inhibition of CYP17A1 activity, suggesting that orteronel might be effective for hormone-dependent breast cancers and estrogen-dependent diseases.	orteronel	12-21	cytochrome P450, family 17, subfamily a, polypeptide 1	Rattus norvegicus	143-150
23371447-6	2013	A new CYP17 inhibitor, with more selective inhibition of 17,20-lyase over 17alpha-hydroxylase, orteronel (TAK-700), is currently undergoing phase III clinical trials in pre- and postchemotherapy CRPC.	orteronel	95-104	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	6-11
24314737-5	2013	Hence, some molecules target the androgen biosynthesis, as abiraterone acetate and orteronel, which are selective inhibitors of the enzyme CYP17.	orteronel	83-92	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	139-144
23371447-6	2013	A new CYP17 inhibitor, with more selective inhibition of 17,20-lyase over 17alpha-hydroxylase, orteronel (TAK-700), is currently undergoing phase III clinical trials in pre- and postchemotherapy CRPC.	orteronel	106-113	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	6-11
23371447-7	2013	In a completed phase II trial in CRPC patients, orteronel demonstrated its efficacy by lowering the levels of circulating androgens, reducing prostate-specific antigen (PSA) levels, and decreasing the levels of circulating tumor cells.	orteronel	48-57	kallikrein related peptidase 3	Homo sapiens	142-173
22249003-7	2012	In this study, we quantified the inhibitory activity and specificity of orteronel for testicular and adrenal androgen production by evaluating its effects on CYP17A1 enzymatic activity, steroid production in monkey adrenal cells and human adrenal tumor cells, and serum levels of dehydroepiandrosterone (DHEA), cortisol, and testosterone after oral dosing in castrated and intact male cynomolgus monkeys.	orteronel	72-81	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	158-165
22249003-12	2012	In terms of human CYP17A1 and human adrenal tumor cells, orteronel inhibited 17,20-lyase activity 5.4 times more potently than 17-hydroxylase activity in cell-free enzyme assays and DHEA production 27 times more potently than cortisol production in human adrenal tumor cells, suggesting greater specificity of inhibition between 17,20-lyase and 17-hydroxylase activities in humans vs monkeys.	orteronel	57-66	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	18-25
22249003-13	2012	In summary, orteronel potently inhibited the 17,20-lyase activity of monkey and human CYP17A1 and reduced serum androgen levels in vivo in monkeys.	orteronel	12-21	cytochrome P450 family 17 subfamily A member 1	Homo sapiens	86-93