LURBINECTEDIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C41H44N4O10S
Molecular Weight	784.874
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12[C@@H]3SC[C@]4(NCCC5=C4NC6=CC=C(OC)C=C56)C(=O)OC[C@H](N1[C@@H](O)[C@@H]7CC8=CC(C)=C(OC)C(O)=C8[C@H]2N7C)C9=C%10OCOC%10=C(C)C(OC(C)=O)=C39

InChI

InChIKey=YDDMIZRDDREKEP-HWTBNCOESA-N

InChI=1S/C41H44N4O10S/c1-17-11-20-12-25-39(48)45-26-14-52-40(49)41(38-22(9-10-42-41)23-13-21(50-5)7-8-24(23)43-38)15-56-37(31(45)30(44(25)4)27(20)32(47)33(17)51-6)29-28(26)36-35(53-16-54-36)18(2)34(29)55-19(3)46/h7-8,11,13,25-26,30-31,37,39,42-43,47-48H,9-10,12,14-16H2,1-6H3/t25-,26-,30+,31+,37+,39-,41+/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28683469 | https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=641468 | https://www.ncbi.nlm.nih.gov/pubmed/28368437 | https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/OncologicDrugsAdvisoryCommittee/UCM563557.pdf

Lurbinectedin (PM-01183) - is a synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. Lurbinectedin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death. Lurbinectedin is a novel anticancer agent currently undergoing late-stage (Phase II /III) clinical evaluation in platinum-resistant ovarian, BRCA1/2-mutated breast and small-cell lung cancer. Lurbinectedin is structurally related to trabectedin and it inhibits active transcription and the DNA repair machinery in tumour cells.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
RNA Polymerase II Transcription 1 Target ID: WP1906 Sources: https://ovariancancernewstoday.com/2017/06/23/ovarian-cancer-therapy-lurbinectedin-by-pharmamar-to-be-marketed-as-zepsyre-once-approved/ \| https://www.pharmamar.com/science-and-innovation/action-mechanisms/ \| https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/OncologicDrugsAdvisoryCommittee/UCM563557.pdf	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Ovarian cancer 157 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28368437 https://clinicaltrials.gov/ct2/show/NCT02421588	Primary		Phase III 656	Unknown Approved Use Unknown
Non-small cell lung cancer 206 Sources: https://clinicaltrials.gov/ct2/show/NCT01951157 http://adisinsight.springer.com/drugs/800030007	Primary		Phase III 656	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
153.8 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24563480	7 mg 1 times / 3 weeks multiple, intravenous dose: 7 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LURBINECTEDIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
532.6 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24563480	7 mg 1 times / 3 weeks multiple, intravenous dose: 7 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LURBINECTEDIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
51.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24563480	7 mg 1 times / 3 weeks multiple, intravenous dose: 7 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LURBINECTEDIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	Disc. AE: Peripheral neuropathy, Myelosuppression... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (>1) Myelosuppression (>1) Neutropenia (>3) Hypoalbuminemia (>3) Febrile neutropenia (>3) Fatigue (>3) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
6.9 mg/m2 1 times / 3 weeks steady, intravenous Highest studied dose Dose: 6.9 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 6.9 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
4 mg/m2 1 times / 3 weeks steady, intravenous MTD Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 4 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	DLT: Thrombocytopenia... Dose limiting toxicities: Thrombocytopenia (grade 4, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	DLT: AST increased, Neutropenia... Dose limiting toxicities: AST increased (grade 4, 2 patients) Neutropenia (grade 4, 2 patients) Fatigue (grade 3, 2 patients) Nausea (grade 2, 2 patients) Vomiting (grade 2, 2 patients) Diarrhea (grade 2, 2 patients) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57

AEs

AE	Significance	Dose	Population
Myelosuppression	>1 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Peripheral neuropathy	>1 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Fatigue	>3 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Febrile neutropenia	>3 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Hypoalbuminemia	>3 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Neutropenia	>3 Disc. AE	3.2 mg/m2 1 times / 3 weeks steady, intravenous Recommended Dose: 3.2 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 3.2 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf	unhealthy, 60 years (range: 40 - 83 years) n = 105 Health Status: unhealthy Condition: small cell lung cancer Age Group: 60 years (range: 40 - 83 years) Sex: M+F Population Size: 105 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf
Thrombocytopenia	grade 4, 1 patient DLT	4 mg/m2 1 times / 3 weeks steady, intravenous MTD Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 4 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
Diarrhea	grade 2, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
Nausea	grade 2, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
Vomiting	grade 2, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
Fatigue	grade 3, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
AST increased	grade 4, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57
Neutropenia	grade 4, 2 patients DLT	5 mg/m2 1 times / 3 weeks steady, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: steady Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57	unhealthy n = 31 Health Status: unhealthy Condition: advanced solid tumors Population Size: 31 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf Page: p. 57

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 OATP1B1 788 OATP1B3 706 OCT1 512 CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP2E1 882	P-gp 1537 OATP1B3 350 OCT1 327 MATE1 135 BCRP 561 BSEP 52 OAT1 326 OAT3 339 OCT2 355	CYP1A2 701

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0	yes
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0	yes
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0	yes
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0	yes

Drug as victim

Target	Modality	Activity
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=52 Page: 52.0	major
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
BSEP 52	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
MATE1 135	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213702s000lbl.pdf#page=11 Page: 11.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213702Orig1s000MultidisciplineR.pdf#page=34 Page: 34.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00DJWD	https://www.aablocks.com/goods/Goods/detail?id=AA00DJWD
AbMole Bioscience	M10037	http://www.abmole.com/products/lurbinectedin.html
BLD Pharm	BD00825727	http://www.bldpharm.com/products/497871-47-3.html
Chem Scene	CS-6323	http://www.chemscene.com/497871-47-3.html
Chemspace	CSSS00161189527	https://chem-space.com/CSSS00161189527
DC Chemicals	DC12502	http://www.dcchemicals.com/product_show-Lurbinectedin.html
DC Chemicals	Lurbinectedin	http://www.dcchemicals.com/product_show-Lurbinectedin.html
Excenen	EX-A4316	https://www.excenen.com/searchresultlist.php?id=EX-A4316
Hairui	LUJL028	http://www.hairuichem.com/en/product/497871-47-3.html
MedChem Express	HY-16293	https://www.medchemexpress.com/Lurbinectedin.html
MolPort	MolPort-046-702-163	https://www.molport.com/shop/molecule-link/MolPort-046-702-163
MuseChem	I013699	https://www.musechem.com/product/I013699.html
Selleck Chemicals	S9603	http://www.selleckchem.com/products/lurbinectedin.html
Smolecule	S533851	http://www.smolecule.com/products/s533851
THE BioTek	bt-274785	https://www.thebiotek.com/product/inhibitors/bt-274785
eNovation Chemicals	D671373	https://www.enovationchem.com/ProductDetails.asp?ProductID=D671373

PubMed

Title	Date	PubMed
Lurbinectedin reduces tumour-associated macrophages and the inflammatory tumour microenvironment in preclinical models.	2017 Aug 22	28683469
Phase II randomized study of PM01183 versus topotecan in patients with platinum-resistant/refractory advanced ovarian cancer.	2017 Jun 1	28368437

Patents

Sample Use Guides

In Vivo Use Guide

Non-Small Cell Lung Cancer: 3.2 mg/m2 Lurbinectedin (PM01183), day 1, 1-hour intravenous, every three weeks

Route of Administration: Intravenous

In Vitro Use Guide

48 hours’ treatment with lurbinectedin (0.3–10 nmol/L) inhibited the proliferation of the ovarian cancer cells of CCC origin in a dose-dependent manner.

Name

Type

Language

LURBINECTEDIN

Official Name

English

LURBINECTEDIN [MI]

Common Name

English

PM1183

Code

English

LURBINECTEDIN [USAN]

Common Name

English

PM-1183

Code

English

TRYPTAMICIDIN

Common Name

English

Lurbinectedin [WHO-DD]

Common Name

English

lurbinectedin [INN]

Common Name

English

(1'R,6R,6AR,7R,13S,14S,16R)-8,14-DIHYDROXY-6',9-DIMETHOXY-4,10,23-TRIMETHYL-19-OXO-2',3',4',6,7,9',12,13,14,16-DECAHYDRO-6AHSPIRO(7,13-AZANO-6,16-(EPITHIOPROPANOOXYMETHANO)(1,3)DIOXOLO(7,8)ISOQUINOLINO(3,2-B)(3)BENZAZOCINE-20,1'-PYRIDO(3,4-B)INDOL)-5-YL

Systematic Name

English

PM-01183

Code

English

SPIRO(6,16-(EPITHIOPROPANOXYMETHANO)-7,13-IMINO-12H-1,3-DIOXOLO(7,8)ISOQUINO(3,2-B)(3)BENZAZOCINE-20,1'-(1H)PYRIDO(3,4-B)INDOL)-19-ONE, 5-(ACETYLOXY)-2',3',4',6,6A,7,9',13,14,16-DECAHYDRO-8,14-DIHYDROXY-6',9-DIMETHOXY-4,10,23-TRIMETHYL-, (1'R,6R,6AR,7R,1

Systematic Name

English

ZEPSYRE

Brand Name

English

PM01183

Code

English

ZEPZELCA

Brand Name

English

LURBINECTEDIN [ORANGE BOOK]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C25760