OLICERIDINE FUMARATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H30N2O2S.C4H4O4
Molecular Weight	502.623
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C\C(O)=O.COC1=C(CNCC[C@]2(CCOC3(CCCC3)C2)C4=NC=CC=C4)SC=C1

InChI

InChIKey=LJQUAERICCVBQQ-CMABEYDLSA-N

InChI=1S/C22H30N2O2S.C4H4O4/c1-25-18-7-15-27-19(18)16-23-13-10-21(20-6-2-5-12-24-20)11-14-26-22(17-21)8-3-4-9-22;5-3(6)1-2-4(7)8/h2,5-7,12,15,23H,3-4,8-11,13-14,16-17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t21-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Molecular Formula	C22H30N2O2S
Molecular Weight	386.551
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://adisinsight.springer.com/drugs/800035617
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23300227

Oliceridine (TRV-130) is a potent μ-opioid receptor agonist. In cell-based assays, TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization. In rodents, TRV130 is potently analgesic while causing less gastrointestinal dysfunction and respiratory suppression than morphine at equianalgesic doses. Oliceridine is being developed by Trevena for the first-line treatment of moderate-to-severe acute postoperative pain. Phase III development is underway for the treatment of postoperative pain in the US. Phase II development is underway for the treatment of acute pain in the US.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mu opioid receptor 231 Target ID: CHEMBL233 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23300227 \| https://www.ncbi.nlm.nih.gov/pubmed/24063433	Agonist 2752		8.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 619 Sources: http://adisinsight.springer.com/drugs/800035617	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
2.29 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.09 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
45.2 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
54.7 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
81.3 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
54 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
127.8 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
117.3 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
239.7 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
183.8 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19.5 pg/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=358	100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
34.8 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
41.4 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
41.9 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.4 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.94 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8.79 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
374.18 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=141	27 mg 12 times / day multiple, intravenous dose: 27 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.29 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
11.14 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
39.1 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
75.6 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
73.8 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
136.6 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
229.3 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
108.2 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
171.59 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
243 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
134 pg × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=358	100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
23.7 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
22.5 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
29.5 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.9 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.2 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
18.1 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.567 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=141	27 mg 12 times / day multiple, intravenous dose: 27 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.56 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.82 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=351	0.25 mg single, intravenous dose: 0.25 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.49 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	1.5 mg single, intravenous dose: 1.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.67 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	3 mg single, intravenous dose: 3 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.64 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=356	4.5 mg single, intravenous dose: 4.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.63 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.07 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=337 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=367	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.62 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=358	100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.07 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.61 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.33 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.77 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=372	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.99 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.34 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=377 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=336	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OLICERIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
23% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210730Orig1s000MultidisciplineR.pdf#page=22			OLICERIDINE plasma	Homo sapiens

Doses

Dose	Population	Adverse events
27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	Disc. AE: Opioid abuse, Opioid type dependence... AEs leading to discontinuation/dose reduction: Opioid abuse Opioid type dependence Respiratory depression (grade 5) Neonatal opioid withdrawal syndrome (grade 4) QT interval prolonged Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf
7 mg single, intravenous Studied dose Dose: 7 mg Route: intravenous Route: single Dose: 7 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24122908/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24122908/	Sources: https://pubmed.ncbi.nlm.nih.gov/24122908/

AEs

AE	Significance	Dose	Population
Opioid abuse	Disc. AE	27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf
Opioid type dependence	Disc. AE	27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf
QT interval prolonged	Disc. AE	27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf
Neonatal opioid withdrawal syndrome	grade 4 Disc. AE	27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf
Respiratory depression	grade 5 Disc. AE	27 mg multiple, intravenous Recommended Dose: 27 mg Route: intravenous Route: multiple Dose: 27 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210730s001lbl.pdf

PubMed

Title	Date	PubMed
How Oliceridine (TRV-130) Binds and Stabilizes a μ-Opioid Receptor Conformational State That Selectively Triggers G Protein Signaling Pathways.	2016-11-22	27778501
A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain.	2016-01	26683109
Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers.	2014-09	24954166
First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers.	2014-03	24122908
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.	2013-10-24	24063433
A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.	2013-03	23300227

Patents

Sample Use Guides

In Vivo Use Guide

Oliceridine dosed at 2mg or 3mg every 3 hours demonstrated a tolerability profile similar to morphine dosed at 4mg every 4 hours, in a randomised, double-blind, placebo-controlled, 48-hour phase IIa/b trial in patients with acute postoperative pain after bunionectomy

Route of Administration: Intravenous

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Wed Apr 02 10:03:00 GMT 2025` Edited by `admin` on `Wed Apr 02 10:03:00 GMT 2025`
Record UNII	0JE2QYQ7CW
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

OLICERIDINE FUMARATE [MI]

Preferred Name

English

OLICERIDINE FUMARATE

Common Name

English

Oliceridine fumarate [WHO-DD]

Common Name

English

6-OXASPIRO(4.5)DECANE-9-ETHANAMINE, N-((3-METHOXY-2-THIENYL)METHYL)-9-(2-PYRIDINYL)-, (9R)-, (2E)-2-BUTENEDIOATE (1:1)

Systematic Name

English

Code System Code Type Description

CAS

1467617-09-9