irinotecan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antineoplastics, topoisomerase I inhibitors 1482 97682-44-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • irinotecan liposome injection
  • onivyde
  • irinotecan liposome
  • irinotecan
  • irinotecan hydrochloride
  • irinotecan hydrochloride hydrate
  • irinotecan hydrochloride trihydrate
  • irinotecan HCl
Irinotecan is a derivative of camptothecin. Camptothecins act as specific inhibitors of the enzyme DNA topoisomerase I. Irinotecan and its active metabolite SN-38 bind reversibly to the topoisomerase I-DNA complex and induce single-strand DNA lesions which block the DNA replication fork and are responsible for the cytotoxicity. Irinotecan is metabolized by carboxylesterase to SN-38. SN-38 is approximately 1000 times as potent as irinotecan as an inhibitor of topoisomerase I purified from human and rodent tumour cell lines.
  • Molecular weight: 586.69
  • Formula: C33H38N4O6
  • CLOGP: 2.43
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 1
  • TPSA: 112.51
  • ALOGS: -3.74
  • ROTB: 5

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 16.70 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.75 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 8 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.51 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 14, 1996 FDA PFIZER INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 2305.15 58.83 851 3948 82713 2270573
Neutropenia 1446.48 58.83 434 4365 21114 2332172
Vomiting 1092.79 58.83 482 4317 71120 2282166
Nausea 802.86 58.83 452 4347 111737 2241549
Disease progression 769.63 58.83 255 4544 16840 2336446
Febrile neutropenia 729.05 58.83 220 4579 10662 2342624
Dehydration 651.05 58.83 241 4558 22054 2331232
Thrombocytopenia 584.67 58.83 214 4585 18917 2334369
Abdominal pain 572.92 58.83 248 4551 34126 2319160
Stomatitis 501.09 58.83 161 4638 9549 2343737
Leukopenia 493.36 58.83 161 4638 10035 2343251
Pyrexia 467.40 58.83 248 4551 53460 2299826
Anaemia 439.09 58.83 207 4592 34585 2318701
Mucosal inflammation 420.42 58.83 122 4677 5102 2348184
Malignant neoplasm progression 419.74 58.83 149 4650 11979 2341307
Asthenia 414.34 58.83 219 4580 46707 2306579
Decreased appetite 401.86 58.83 184 4615 28707 2324579
Neuropathy peripheral 390.02 58.83 139 4660 11293 2341993
General physical health deterioration 364.81 58.83 140 4659 13999 2339287
Fatigue 347.98 58.83 242 4557 84631 2268655
Hypertension 308.67 58.83 151 4648 27210 2326076
Bone marrow failure 295.75 58.83 95 4704 5591 2347695
Pulmonary embolism 269.25 58.83 121 4678 17962 2335324
Sepsis 238.47 58.83 112 4687 18376 2334910
Off label use 233.07 58.83 180 4619 73418 2279868
Neutrophil count decreased 227.94 58.83 81 4718 6486 2346800
Palmar-plantar erythrodysaesthesia syndrome 225.78 58.83 72 4727 4129 2349157
Metastases to liver 215.70 58.83 64 4735 2877 2350409
Neurotoxicity 212.90 58.83 59 4740 2071 2351215
Polyneuropathy 204.92 58.83 55 4744 1708 2351578
Proteinuria 187.32 58.83 57 4742 2793 2350493
Hypokalaemia 183.27 58.83 79 4720 10575 2342711
Haematotoxicity 177.07 58.83 45 4754 1122 2352164
Pancytopenia 168.19 58.83 76 4723 11376 2341910
Peripheral sensory neuropathy 167.59 58.83 42 4757 988 2352298
Hypomagnesaemia 167.30 58.83 51 4748 2513 2350773
Haemoglobin decreased 165.70 58.83 87 4712 18064 2335222
Neoplasm progression 163.50 58.83 58 4741 4610 2348676
Dermatitis acneiform 162.09 58.83 39 4760 770 2352516
Dyspnoea 159.19 58.83 149 4650 78584 2274702
White blood cell count decreased 154.13 58.83 83 4716 18125 2335161
Ileus 153.72 58.83 46 4753 2126 2351160
Colorectal cancer metastatic 153.66 58.83 29 4770 162 2353124
Dysarthria 153.58 58.83 60 4739 6242 2347044
Intestinal obstruction 147.85 58.83 53 4746 4340 2348946
Ascites 145.80 58.83 56 4743 5564 2347722
Death 145.43 58.83 144 4655 81324 2271962
Interstitial lung disease 141.11 58.83 60 4739 7752 2345534
Constipation 138.16 58.83 82 4717 21547 2331739
Alopecia 136.86 58.83 82 4717 21919 2331367
Pneumonia 130.80 58.83 109 4690 49187 2304099
Chills 126.29 58.83 69 4730 15483 2337803
Posterior reversible encephalopathy syndrome 122.91 58.83 40 4759 2440 2350846
Hypophagia 115.07 58.83 43 4756 3957 2349329
Platelet count decreased 114.30 58.83 65 4734 15748 2337538
Deep vein thrombosis 112.29 58.83 60 4739 12872 2340414
Device related infection 112.20 58.83 40 4759 3219 2350067
Speech disorder 111.27 58.83 48 4751 6416 2346870
Gastrointestinal toxicity 110.97 58.83 27 4772 559 2352727
Oesophagitis 110.24 58.83 35 4764 1971 2351315
Dysphagia 110.03 58.83 59 4740 12746 2340540
Infusion related reaction 109.83 58.83 54 4745 9742 2343544
Urinary tract infection 109.23 58.83 80 4719 29862 2323424
Therapeutic product effect incomplete 109.05 58.83 55 4744 10476 2342810
Hypotension 107.92 58.83 82 4717 32354 2320932
Skin toxicity 107.79 58.83 28 4771 762 2352524
Epistaxis 106.93 58.83 53 4746 9726 2343560
Toxicity to various agents 105.01 58.83 81 4718 32673 2320613
Neutropenic sepsis 104.00 58.83 31 4768 1411 2351875
Intestinal perforation 101.53 58.83 32 4767 1759 2351527
Paraesthesia 101.48 58.83 68 4731 22020 2331266
Malaise 98.42 58.83 98 4701 55487 2297799
Weight decreased 94.94 58.83 72 4727 28299 2324987
Proctalgia 92.88 58.83 24 4775 639 2352647
Paronychia 92.44 58.83 25 4774 797 2352489
Septic shock 91.53 58.83 43 4756 7011 2346275
Small intestinal obstruction 90.85 58.83 31 4768 2189 2351097
Abdominal pain upper 89.60 58.83 63 4736 22037 2331249
Mucosal toxicity 88.96 58.83 16 4783 65 2353221
Product use in unapproved indication 88.95 58.83 49 4750 11151 2342135
Hyponatraemia 88.87 58.83 52 4747 13273 2340013
Metastases to lung 86.09 58.83 28 4771 1703 2351583
Multiple organ dysfunction syndrome 85.26 58.83 42 4757 7599 2345687
Nephroblastoma 81.64 58.83 13 4786 19 2353267
Enteritis 81.16 58.83 24 4775 1062 2352224
Hypocalcaemia 80.75 58.83 33 4766 3850 2349436
Colorectal cancer 80.65 58.83 18 4781 251 2353035
Colon cancer 79.95 58.83 27 4772 1846 2351440
Acute kidney injury 78.18 58.83 64 4735 28058 2325228
Drug ineffective 77.51 58.83 117 4682 101507 2251779
Cholangitis 77.17 58.83 22 4777 854 2352432
Infection 76.80 58.83 53 4746 17976 2335310
Rash 75.43 58.83 88 4711 59470 2293816
Metastases to meninges 73.81 58.83 18 4781 376 2352910
Seizure 72.91 58.83 58 4741 24408 2328878
Blood creatinine increased 72.58 58.83 42 4757 10491 2342795
Metastases to peritoneum 71.12 58.83 18 4781 440 2352846
Chest pain 69.86 58.83 60 4739 28077 2325209
Hypertensive crisis 68.57 58.83 26 4773 2487 2350799
Hypersensitivity 68.31 58.83 55 4744 23538 2329748
Blood alkaline phosphatase increased 67.17 58.83 34 4765 6511 2346775
Large intestine perforation 65.13 58.83 21 4778 1241 2352045
Disease recurrence 63.89 58.83 27 4772 3424 2349862
Dysphonia 62.23 58.83 32 4767 6332 2346954

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 3225.58 54.44 1230 5866 52622 1687063
Neutropenia 1699.89 54.44 585 6511 17675 1722010
Disease progression 973.70 54.44 384 6712 16879 1722806
Febrile neutropenia 944.11 54.44 334 6762 10766 1728919
Vomiting 893.57 54.44 459 6637 37856 1701829
Dehydration 813.58 54.44 340 6756 17318 1722367
Decreased appetite 793.09 54.44 365 6731 23506 1716179
Nausea 779.39 54.44 463 6633 50733 1688952
Stomatitis 668.95 54.44 216 6880 5188 1734497
Pyrexia 635.97 54.44 393 6703 46007 1693678
Abdominal pain 591.09 54.44 289 6807 21201 1718484
Leukopenia 588.29 54.44 220 6876 8260 1731425
Neuropathy peripheral 555.35 54.44 216 6880 9037 1730648
Asthenia 541.85 54.44 320 6776 34350 1705335
General physical health deterioration 531.17 54.44 231 6865 12887 1726798
Thrombocytopenia 525.56 54.44 266 6830 20983 1718702
Interstitial lung disease 472.91 54.44 195 6901 9501 1730184
Anaemia 451.97 54.44 269 6827 29188 1710497
Fatigue 443.93 54.44 326 6770 50455 1689230
Pulmonary embolism 417.09 54.44 195 6901 12864 1726821
Mucosal inflammation 401.10 54.44 138 6958 4031 1735654
Malignant neoplasm progression 363.19 54.44 182 6914 13976 1725709
Hypertension 349.13 54.44 197 6899 19251 1720434
Metastases to liver 343.84 54.44 106 6990 2161 1737524
Off label use 341.48 54.44 250 6846 38321 1701364
Alopecia 298.89 54.44 108 6988 3645 1736040
Palmar-plantar erythrodysaesthesia syndrome 298.43 54.44 106 6990 3401 1736284
Intestinal obstruction 294.64 54.44 105 6991 3402 1736283
Neoplasm progression 286.55 54.44 101 6995 3166 1736519
Dermatitis acneiform 274.38 54.44 75 7021 977 1738708
Neutrophil count decreased 271.45 54.44 115 6981 5966 1733719
Bone marrow failure 268.08 54.44 109 6987 5091 1734594
Sepsis 262.50 54.44 164 6932 19274 1720411
Weight decreased 255.67 54.44 171 6925 22582 1717103
Hypokalaemia 246.69 54.44 109 6987 6265 1733420
Cholinergic syndrome 219.70 54.44 43 7053 97 1739588
Epistaxis 219.14 54.44 109 6987 8197 1731488
White blood cell count decreased 218.88 54.44 127 6969 13022 1726663
Colorectal cancer metastatic 217.91 54.44 47 7049 199 1739486
Ileus 215.87 54.44 76 7020 2370 1737315
Haemoglobin decreased 212.45 54.44 137 6959 16977 1722708
Proteinuria 204.68 54.44 76 7020 2768 1736917
Metastases to lung 200.19 54.44 64 7032 1471 1738214
Pneumonia 191.11 54.44 194 6902 45988 1693697
Deep vein thrombosis 187.05 54.44 104 6992 9816 1729869
Colorectal cancer 186.82 54.44 46 7050 383 1739302
Constipation 185.90 54.44 120 6976 14880 1724805
Gastrointestinal toxicity 185.47 54.44 45 7051 350 1739335
Septic shock 183.57 54.44 96 7000 8013 1731672
Acute kidney injury 180.63 54.44 166 6930 34778 1704907
Small intestinal obstruction 173.61 54.44 60 7036 1767 1737918
Dyspnoea 171.81 54.44 194 6902 51865 1687820
Skin toxicity 166.87 54.44 45 7051 554 1739131
Hypomagnesaemia 165.49 54.44 60 7036 2038 1737647
Paronychia 158.88 54.44 43 7053 537 1739148
Ascites 158.24 54.44 77 7019 5509 1734176
Neurotoxicity 156.35 54.44 57 7039 1967 1737718
Chills 155.92 54.44 98 6998 11589 1728096
Neutropenic sepsis 153.46 54.44 52 7044 1440 1738245
Haematotoxicity 150.23 54.44 46 7050 912 1738773
Hiccups 146.13 54.44 50 7046 1427 1738258
Abdominal pain upper 146.11 54.44 92 7004 10909 1728776
Hypotension 145.60 54.44 137 6959 29517 1710168
Necrotising fasciitis 140.48 54.44 40 7056 609 1739076
Rash 137.40 54.44 150 6946 38543 1701142
Intestinal perforation 134.04 54.44 48 7048 1571 1738114
Abdominal pain lower 127.80 54.44 43 7053 1164 1738521
Peritonitis 122.72 54.44 52 7044 2687 1736998
Peripheral sensory neuropathy 120.92 54.44 38 7058 823 1738862
Hyperbilirubinaemia 114.50 54.44 47 7049 2240 1737445
Cholangitis 112.74 54.44 39 7057 1150 1738535
Platelet count decreased 110.33 54.44 91 7005 16432 1723253
Paraesthesia 106.22 54.44 74 7022 10377 1729308
Oesophagitis 106.21 54.44 41 7055 1660 1738025
Skin reaction 105.69 54.44 37 7059 1131 1738554
Malaise 103.72 54.44 114 6982 29451 1710234
C-reactive protein increased 103.49 54.44 59 7037 5826 1733859
Atrial fibrillation 102.50 54.44 84 7012 15027 1724658
Device related infection 101.07 54.44 43 7053 2243 1737442
Renal failure 101.00 54.44 94 7002 19923 1719762
Hepatic failure 100.64 54.44 58 7038 5845 1733840
Pancytopenia 96.19 54.44 72 7024 11285 1728400
Colitis 95.95 54.44 50 7046 4130 1735555
Colitis microscopic 94.94 54.44 26 7070 340 1739345
Pain 93.83 54.44 103 6993 26554 1713131
Therapeutic product effect incomplete 91.46 54.44 53 7043 5395 1734290
Infection 90.78 54.44 72 7024 12288 1727397
Hypersensitivity 90.20 54.44 67 7029 10377 1729308
Respiratory failure 88.77 54.44 76 7020 14429 1725256
Hypophagia 86.52 54.44 44 7052 3453 1736232
Colon cancer 85.52 54.44 36 7060 1828 1737857
Hypoalbuminaemia 83.41 54.44 33 7063 1427 1738258
Acne 83.22 54.44 35 7061 1773 1737912
Tachycardia 83.10 54.44 69 7027 12559 1727126
Large intestine perforation 82.83 54.44 31 7065 1151 1738534
Hepatotoxicity 82.75 54.44 41 7055 3043 1736642
Dyspepsia 82.36 54.44 48 7048 4937 1734748
Disseminated intravascular coagulation 82.28 54.44 43 7053 3571 1736114
Subileus 77.91 54.44 24 7072 485 1739200
Colon cancer metastatic 77.91 54.44 22 7074 324 1739361
Subclavian vein thrombosis 76.73 54.44 19 7077 162 1739523
Oedema peripheral 76.41 54.44 72 7024 15478 1724207
Hyponatraemia 76.05 54.44 57 7039 8943 1730742
Pneumocystis jirovecii pneumonia 75.99 54.44 36 7060 2420 1737265
Thrombosis 75.78 54.44 53 7043 7468 1732217
Rectal haemorrhage 75.12 54.44 47 7049 5495 1734190
Haematochezia 74.95 54.44 45 7051 4887 1734798
Tumour lysis syndrome 74.30 54.44 32 7064 1719 1737966
Polyneuropathy 74.23 54.44 32 7064 1723 1737962
Hyperglycaemia 73.04 54.44 45 7051 5120 1734565
Abdominal distension 71.03 54.44 48 7048 6396 1733289
Enteritis 69.80 54.44 26 7070 952 1738733
Anal fissure 69.29 54.44 20 7076 320 1739365
Death 67.93 54.44 170 6926 87273 1652412
Mouth ulceration 67.73 54.44 30 7066 1725 1737960
Blood creatinine increased 67.41 54.44 64 7032 13882 1725803
Conjunctivitis 66.60 54.44 29 7067 1600 1738085
Lethargy 66.32 54.44 48 7048 7136 1732549
Coagulopathy 65.91 54.44 34 7062 2747 1736938
Anaemia of malignant disease 65.51 54.44 14 7082 56 1739629
Pneumonitis 65.46 54.44 38 7058 3877 1735808
Dysarthria 64.80 54.44 42 7054 5217 1734468
Ejection fraction decreased 63.67 54.44 31 7065 2214 1737471
Dysphagia 63.65 54.44 54 7042 10114 1729571
Klebsiella infection 63.08 54.44 23 7073 792 1738893
Posterior reversible encephalopathy syndrome 62.73 54.44 27 7069 1448 1738237
Dry skin 61.98 54.44 36 7060 3676 1736009
Atelectasis 61.83 54.44 29 7067 1905 1737780
Urinary tract infection 61.67 54.44 53 7043 10100 1729585
Condition aggravated 61.33 54.44 74 7022 21076 1718609
Lung disorder 60.92 54.44 40 7056 5079 1734606
Leukoencephalopathy 59.78 54.44 22 7074 778 1738907
Ill-defined disorder 59.50 54.44 28 7068 1853 1737832
Jaundice 59.38 54.44 42 7054 6020 1733665
Chronic myeloid leukaemia 58.91 54.44 21 7075 677 1739008
Circulatory collapse 58.89 54.44 34 7062 3433 1736252
Tumour haemorrhage 58.80 54.44 20 7076 559 1739126
Blood bilirubin increased 58.47 54.44 42 7054 6168 1733517
Candida infection 58.43 54.44 28 7068 1930 1737755
Cachexia 58.15 54.44 23 7073 993 1738692
Proctalgia 58.07 54.44 21 7075 706 1738979
Melaena 57.87 54.44 39 7057 5171 1734514
Proteus infection 57.32 54.44 14 7082 112 1739573
Hypovolaemic shock 57.07 54.44 22 7074 886 1738799
Gastrointestinal haemorrhage 56.95 54.44 59 7037 14208 1725477
Large intestinal obstruction 56.14 54.44 16 7080 244 1739441
Rectal cancer 55.90 54.44 19 7077 530 1739155
Clostridial infection 54.84 54.44 20 7076 689 1738996
Venous thrombosis 54.82 54.44 20 7076 690 1738995

Pharmacologic Action:

SourceCodeDescription
ATC L01XX19 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA EPC N0000175609 Topoisomerase Inhibitor
FDA MoA N0000000176 Topoisomerase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50266 prodrug
MeSH PA D059004 Topoisomerase I Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Secondary malignant neoplasm of pancreas indication 94459006
Metastasis from malignant tumor of colon indication 314998002
Adenocarcinoma of pancreas indication 700423003 DOID:4074
Astrocytoma, anaplastic off-label use 55353007 DOID:3078
Ewing's sarcoma off-label use 76909002 DOID:3369
Small cell carcinoma of lung off-label use 254632001 DOID:5409
Non-small cell lung cancer off-label use 254637007 DOID:3908
Glioblastoma multiforme of brain off-label use 276828006 DOID:3073
Hyperbilirubinemia contraindication 14783006 DOID:2741
Dehydration contraindication 34095006
Diarrhea contraindication 62315008
Interstitial pneumonia contraindication 64667001
Intestinal obstruction contraindication 81060008 DOID:8437
Kidney disease contraindication 90708001 DOID:557
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Sepsis syndrome contraindication 238150007
Renal dialysis contraindication 265764009
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Thromboembolic disorder contraindication 371039008
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001
UGT1A1*28 polymorphism contraindication 430235005

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.46 acidic
pKa2 9.25 Basic
pKa3 2.69 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/5ML (20MG/ML) CAMPTOSAR PFIZER INC N020571 June 14, 1996 RX INJECTABLE INJECTION 6403569 April 28, 2020 USE IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN FOR THE TREATMENT OF METASTATIC COLORECTAL CANCER WHERE THE DOSE OF LEUCOVORIN IS AT LEAST 200MG PER SQUARE METER
40MG/2ML (20MG/ML) CAMPTOSAR PFIZER INC N020571 June 14, 1996 RX INJECTABLE INJECTION 6403569 April 28, 2020 USE IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN FOR THE TREATMENT OF METASTATIC COLORECTAL CANCER WHERE THE DOSE OF LEUCOVORIN IS AT LEAST 200MG PER SQUARE METER
100MG/5ML (20MG/ML) CAMPTOSAR PFIZER INC N020571 June 14, 1996 RX INJECTABLE INJECTION 6794370 May 1, 2020 USE OF IRINOTECAN IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN FOR THE TREATMENT OF METASTATIC COLORECTAL CANCER
40MG/2ML (20MG/ML) CAMPTOSAR PFIZER INC N020571 June 14, 1996 RX INJECTABLE INJECTION 6794370 May 1, 2020 USE OF IRINOTECAN IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN FOR THE TREATMENT OF METASTATIC COLORECTAL CANCER
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 8703181 May 2, 2025 TREATMENT OF PANCREATIC CANCER
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9730891 May 2, 2025 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9339497 June 12, 2033 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9364473 June 12, 2033 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN, IN A PATIENT HOMOZYGOUS FOR THE UGT1A1*28 ALLELE
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9452162 June 12, 2033 TREATMENT OF PANCREATIC CANCER THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9492442 June 12, 2033 TREATMENT OF EXOCRINE PANCREATIC CANCER THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9492442 June 12, 2033 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9492442 June 12, 2033 TREATMENT OF PANCREATIC CANCER THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9717724 June 12, 2033 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS 9717724 June 12, 2033 TREATMENT OF METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED ON GEMCITABINE-BASED THERAPY, IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN, IN A PATIENT NOT HOMOZYGOUS FOR THE UGT1A1*28 ALLELE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 43MG BASE/10ML (EQ 4.3MG BASE/ML) ONIVYDE IPSEN INC N207793 Oct. 22, 2015 RX INJECTABLE, LIPOSOMAL INTRAVENOUS Oct. 22, 2022 FOR USE IN COMBINATION WITH 5-FLUOROURACIL AND LEUCOVORIN, FOR THE TREATMENT OF PATIENTS WITH METASTATIC ADENOCARCINOMA OF THE PANCREAS THAT HAS PROGRESSED FOLLOWING GEMCITABINE-BASED THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
DNA topoisomerase 1 Enzyme INHIBITOR DRUGBANK CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 6.66 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.34 DRUG MATRIX
Interstitial collagenase Enzyme IC50 5.22 DRUG MATRIX
Multidrug resistance-associated protein 4 Transporter WOMBAT-PK
ATP-binding cassette sub-family G member 2 Transporter WOMBAT-PK
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
Canalicular multispecific organic anion transporter 1 Transporter WOMBAT-PK
Multidrug resistance protein 1 Transporter WOMBAT-PK
Solute carrier family 22 member 3 Transporter IC50 4.13 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.68 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 5.57 CHEMBL
Acetylcholinesterase Enzyme Ki 7.30 CHEMBL
Multidrug and toxin extrusion protein 2 Transporter IC50 5.10 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.68 CHEMBL
Acetylcholinesterase Enzyme Ki 7.58 CHEMBL

External reference:

IDSource
D000077146 MESH_DESCRIPTOR_UI
4024027 VUID
N0000022032 NUI
C0123931 UMLSCUI
D01061 KEGG_DRUG
7673326042 UNII
6694 INN_ID
136572-09-3 SECONDARY_CAS_RN
108783005 SNOMEDCT_US
4024027 VANDF
d04026 MMSL
4918 MMSL
51499 RXNORM
372538008 SNOMEDCT_US
005262 NDDF
CHEMBL481 ChEMBL_ID
DB00762 DRUGBANK_ID
CHEMBL541887 ChEMBL_ID
CHEMBL1200512 ChEMBL_ID
CP0 PDB_CHEM_ID
CHEBI:80630 CHEBI
CHEMBL3989514 ChEMBL_ID
60838 PUBCHEM_CID
6823 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Camptosar HUMAN PRESCRIPTION DRUG LABEL 1 0009-7529 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 20 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9583 INJECTION 20 mg INTRAVENOUS ANDA 18 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9701 INJECTION 20 mg INTRAVENOUS ANDA 18 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9702 INJECTION 20 mg INTRAVENOUS ANDA 18 sections
Onivyde HUMAN PRESCRIPTION DRUG LABEL 1 15054-0043 INJECTION, POWDER, FOR SOLUTION 4.30 mg INTRAVENOUS NDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 16714-725 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 16714-726 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 25021-230 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 45963-614 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50742-401 INJECTION 40 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50742-402 INJECTION 100 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 59923-702 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 59923-714 INJECTION 20 mg INTRAVENOUS ANDA 17 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 59923-715 INJECTION 20 mg INTRAVENOUS ANDA 17 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 59923-716 INJECTION 20 mg INTRAVENOUS ANDA 17 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60505-6128 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61703-349 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63323-193 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67184-0511 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67184-0512 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 67184-0513 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68001-284 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan hydrochloide HUMAN PRESCRIPTION DRUG LABEL 1 68083-381 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68083-382 INJECTION 20 mg INTRAVENOUS ANDA 19 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72485-211 INJECTION 20 mg INTRAVENOUS ANDA 18 sections
Irinotecan Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72485-212 INJECTION 20 mg INTRAVENOUS ANDA 18 sections