Lapatinib
Small molecule targets ABCB1, CYP2C8, CYP3A4, EGF, EGFR, ERBB2 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | EU (EMA) | Tyverb | — | 2008-06-10 | europa.eu ↗ |
Trials 246 · started per year
Also used as a comparator or background therapy in 32 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 01 trial | ||||||
| Phase 0 | NCT01875666 Comparator | Aug 2013 → Dec 2016 | breast neoplasm | UNC Lineberger Comprehensive Cancer Center | Completed | No outcome recorded |
| Phase 16 trials | ||||||
| Phase 1 | NCT01471847 Comparator | Feb → Jun 2012 | breast cancer | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01304784 Background | Jan 2011 → Apr 2014 | carcinoma | Merrimack Pharmaceuticals | Completed | No outcome recorded |
| Phase 1 | NCT01199367 Background | Dec 2010 → Dec 2012 | breast cancer | Kyowa Kirin, Inc. | Terminated | No outcome recorded |
| Phase 1 | NCT00807859 Background | Mar 2009 → Feb 2014 | female breast carcinoma, metastatic malignant neoplasm | Amgen | Completed | No outcome recorded |
| Phase 1 | NCT00682279 Comparator | Sep 2008 → Mar 2011 | cancer | GlaxoSmithKline | Withdrawn | No outcome recorded |
| Phase 1 | NCT00367471 Comparator | Dec 2006 → Dec 2010 | breast cancer | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 1/21 trial | ||||||
| Phase 1/2 | NCT02422199 Comparator | May 2015 → Oct 2016 | HER2 positive breast carcinoma | Jiangsu HengRui Medicine Co., Ltd. | Unknown | No outcome recorded |
| Phase 210 trials | ||||||
| Phase 2 | NCT02338245 Comparator | Dec 2014 → May 2016 | breast cancer | ASLAN Pharmaceuticals | Completed | No outcome recorded |
| Phase 2 | NCT02294786 Background | Dec 2014 → Oct 2017 | cancer | Novartis Pharmaceuticals | Terminated | No outcome recorded |
| Phase 2 | NCT02213042 Comparator | Oct 2014 → Jun 2020 | breast cancer | Novartis Pharmaceuticals | Terminated | No outcome recorded |
| Phase 2 | NCT01711658 Comparator | Mar 2013 → Dec 2020 | head and neck carcinoma | Radiation Therapy Oncology Group | Completed | No outcome recorded |
| Phase 2 | NCT01306045 Comparator | Feb 2011 → Feb 2014 | non-small cell lung carcinoma, small cell lung carcinoma, thymic carcinoma | National Cancer Institute (NCI) | Completed | No outcome recorded |
| Phase 2 | NCT01068704 Comparator | Jun → Dec 2010 | breast cancer | Bristol-Myers Squibb | Completed | No outcome recorded |
| Phase 2 | NCT01128543 Comparator | Apr 2009 → Mar 2012 | cancer | GlaxoSmithKline | Completed | No outcome recorded |
| Phase 2 | NCT00777101 Comparator | Feb 2009 → Mar 2011 | breast cancer | Puma Biotechnology, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00826267 Comparator | Jan 2009 → Aug 2011 | breast neoplasm | Boehringer Ingelheim | Completed | No outcome recorded |
| Phase 2 | NCT00657137 Background | Apr 2008 → Sep 2009 | breast cancer | Tragara Pharmaceuticals, Inc. | Terminated | No outcome recorded |
| Phase 2/32 trials | ||||||
| Phase 2/3 | NCT03500380 Comparator | Apr 2018 → Jul 2024 | HER2 positive breast carcinoma | RemeGen Co., Ltd. | Unknown | No outcome recorded |
| Phase 2/3 | NCT01426880 Background | Aug 2011 → May 2013 | HER2 positive breast carcinoma, breast mucinous carcinoma, female breast carcinoma, inflammatory breast carcinoma +1 | GBG Forschungs GmbH | Completed | No outcome recorded |
| Phase 311 trials | ||||||
| Phase 3 | NCT06313983 Comparator | Jan 2022 → Dec 2025 overdue | breast cancer | Tianjin Hemay Pharmaceutical Co., Ltd | Recruiting | No outcome recorded |
| Phase 3 | NCT03523585 Comparator | Aug 2018 → Jun 2022 | breast cancer | Daiichi Sankyo | Completed | No outcome recorded |
| Phase 3 | NCT04185649 Comparator | Jul 2018 → Jul 2020 | HER2 positive breast carcinoma | Bio-Thera Solutions | Unknown | No outcome recorded |
| Phase 3 | NCT03262935 Comparator | Dec 2017 → Mar 2021 | breast cancer | Byondis B.V. | Completed | No outcome recorded |
| Phase 3 | NCT03080805 Comparator | May 2017 → Mar 2019 | HER2 positive breast carcinoma | Jiangsu HengRui Medicine Co., Ltd. | Unknown | No outcome recorded |
| Phase 3 | NCT03084939 Comparator | Apr 2017 → Nov 2018 | breast cancer | Hoffmann-La Roche | Completed | No outcome recorded |
| Phase 3 | NCT01808573 Comparator | Mar 2013 → Sep 2018 | HER2 positive breast carcinoma | Puma Biotechnology, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT01160211 Comparator | May 2011 → Mar 2016 | breast neoplasm | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 3 | NCT00829166 Comparator | Feb 2009 → Jul 2012 | breast cancer | Hoffmann-La Roche | Completed | No outcome recorded |
| Phase 3 | NCT00667251 Comparator | Oct 2008 → Aug 2012 | female breast carcinoma | Novartis Pharmaceuticals | Completed | No outcome recorded |
| Phase 3 | NCT00688194 Comparator | May 2008 → May 2013 | breast cancer | Gruppo Italiano Mammella (GIM) | Unknown | No outcome recorded |
| Phase not applicable1 trial | ||||||
| — | NCT02208583 Comparator | Jun 2014 → Dec 2016 | hormone-resistant prostate carcinoma | Tianjin Medical University Cancer Institute and Hospital | Unknown | No outcome recorded |
Evidence & citations 16 cited values
Every value below carries the sentence it was read from. 281 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Lapatinib | “The microdevices will dwell in the tumor tissue for a time window of 2-4 hours to allow time for tissue effects of the drugs (Temozolomide, Lomustine, Irinotecan, Carboplatin,...” NCT04135807 ↗273“Participants who have erythroblastic leukemia viral oncogene homolog 2 (ERBB2) gene mutation will receive a drug called lapatinib, which inhibits some proteins that are thought...” NCT02208583 ↗ “This study was conducted to determine the safety and pharmacokinetics (PK) of the combination of lapatinib, a Her1 and 2 inhibitor, and everolimus and to describe its...” PMID 24057042 ↗ Sep 2013 “Lapatinib (GW572016) is an orally active small molecule that reversibly inhibits ErbB1 and ErbB2 tyrosine kinases” NCT02394496 ↗ “Tablets contain 405mg of lapatinib ditosylate monohydrate, equivalent to 250mg lapatinib free base per tablet.” NCT00371488 ↗ “Lapatinib is an oral, small molecule, dual tyrosine kinase inhibitor of HER2 and EGFR.” NCT00486668 ↗ “Subjects will self-administer lapatinib 1500 mg orally once daily.” NCT00462956 ↗ “Lapatinib 750 mg/day p.o. continuously for 18 weeks” NCT01426880 ↗ “Drug: Gefitinib Drug: Lapatinib Drug: Everolimus” NCT03768375 ↗ “Lapatinib either at 750, 1000, 1250 or 1500 mgs” NCT00169533 ↗ “Lapatinib was administered once daily orally.” NCT00528281 ↗ “Ixabepilone, Lapatinib, Lomustine” NCT02788201 ↗ “Irinotecan Lapatinib Lomustine” NCT02551718 ↗ “GW572016 (lapatinib)” NCT00073008 ↗ “Lapatinib 500 mg PO” NCT00206427 ↗ “Lapatinib (Lap)” NCT03262935 ↗ “Lapatinib” NCT00098605 ↗ “Lapatinib” NCT02142036 ↗ |
| Known as | GW572016 | “A Randomized, Multicenter, Open-label, Phase III Study of Lapatinib (GW572016) in Combination With Weekly Paclitaxel Versus Weekly Paclitaxel Alone in the Second Line Treatment...” NCT00486954 ↗21“The primary objective of this phase I study is to determine the safety, tolerability and optimal tolerated regimen of GW572016 when combined with gemcitabine and with the...” NCT00439179 ↗ “To determine the response rate (complete response and partial response) of tamoxifen (tamoxifen citrate) and GW572016 (lapatinib ditosylate) in women with hormone refractory,...” NCT00118157 ↗ “Lapatinib (GW572016) is an orally active small molecule that reversibly inhibits ErbB1 and ErbB2 tyrosine kinases” NCT02394496 ↗ “Lapatinib (GW572016) is a potent small molecule, reversible inhibitor of both EGFR and ErbB2 tyrosine kinases” NCT00367471 ↗ “Adjuvant Lapatinib (GW572016) in Women With Early-Stage ErbB2 Overexpressing Breast Cancer” NCT00374322 ↗ “Participants will take GW572016 by mouth daily each cycle (cycles 28 days in length)” NCT00295243 ↗ “Oral Lapatinib (GW572016) as Single Agent, Second-Line Therapy” NCT00044343 ↗ “dual tyrosine kinase inhibitor GW572016 (Lapatinib)” NCT00820924 ↗ “oral topotecan (SK&F-104864); lapatinib (GW572016)” NCT00682279 ↗ “oral GW572016 as Single Agent Therapy” NCT00051103 ↗ “Lapatinib (GW572016) oral tablets” NCT00259987 ↗ “Lapatinib (GW572016) oral tablets” NCT00281658 ↗ “Lapatinib (GW572016, Tykerb)” NCT01172223 ↗ “lapatinib (GW572016) 1500 mg” NCT00347919 ↗ “GW572016 (Lapatinib)” NCT00075270 ↗ “lapatinib (GW572016)” NCT00316407 ↗ “lapatinib (GW572016)” NCT00430781 ↗ “lapatinib (GW572016)” NCT00078572 ↗ |
| Known as | GW572016 ditosylate salt | “GW572016 ditosylate salt (lapatinib) will be given as 250 mg tablets via oral route” NCT00359190 ↗ |
| Known as | LAP | “Lapatinib ditosylate (LAP), a dual anti-epidermal growth factor receptor (EGFR) and anti-HER2 tyrosine kinase inhibitor with preclinical activity against GC, has been approved...” PMID 25694417 ↗ Feb 2015 |
| Known as | Lapatinib (Lap) | “Lapatinib (Lap)” NCT03262935 ↗ |
| Known as | Lapatinib (Tykerb) | “Lapatinib (Tykerb)” NCT02158507 ↗1“Lapatinib: Tykerb” NCT00486954 ↗ |
| Known as | lapatinib ditosylate | “Determine the maximum tolerated dose and recommended doses of lapatinib ditosylate when administered with gemcitabine hydrochloride and cisplatin, and determine on the basis of...” NCT00623064 ↗13“PRIMARY OBJECTIVES: I. The primary objective of this study is to estimate the objective response rate (complete response \[CR\] + partial response \[PR\]) in patients with...” NCT00114283 ↗ “This phase II trial studies the effectiveness of lapatinib ditosylate (lapatinib) together with trastuzumab in treating patients with HER2-negative breast cancer that carries...” NCT01557764 ↗ “lapatinib (lapatinib ditosylate) therapy at the dose of 1000 mg” NCT00555152 ↗ “concurrent lapatinib (lapatinib ditosylate) and radiotherapy” NCT01868503 ↗ “Patients receive oral lapatinib ditosylate once daily.” NCT00967031 ↗ “lapatinib (lapatinib ditosylate)” NCT01705340 ↗ “Drug: lapatinib ditosylate” NCT00688194 ↗ “Drug: lapatinib ditosylate” NCT00098605 ↗ “Drug: lapatinib ditosylate” NCT00316875 ↗ “Drug: Lapatinib Ditosylate” NCT00770809 ↗ “Drug: lapatinib ditosylate” NCT01123473 ↗ “Drug: lapatinib ditosylate” NCT00482391 ↗ “Drug: Lapatinib Ditosylate” NCT00118157 ↗ |
| Known as | Lapatinib ditosylate monohydrate | “Tablets contain 405mg of lapatinib ditosylate monohydrate, equivalent to 250mg lapatinib free base per tablet.” NCT00371488 ↗1“Each tablet contained 405mg of Lapatinib ditosylate monohydrate, equivalent to 250mg Lapatinib free base” NCT02294786 ↗ |
| Known as | lapatinib free base | “Tablets contain 405mg of lapatinib ditosylate monohydrate, equivalent to 250mg lapatinib free base per tablet.” NCT00371488 ↗ |
| Known as | lapatinib tosylate | “oral lapatinib tosylate” NCT00688194 ↗ |
| Known as | Tykerb | “This was an open-label, single-arm, multi-center, Phase II study to determine the activity of nab-paclitaxel plus lapatinib (TYKERB) in the first and second-line setting in...” NCT00709761 ↗7“TRYHARD: A Phase II, Randomized, Double Blind, Placebo-Controlled Study of Lapatinib (Tykerb®) for Non-HPV Locally Advanced Head and Neck Cancer With Concurrent Chemoradiation” NCT01711658 ↗ “GlaxoSmithKline markets the drug lapatinib under the propriety names Tykerb (mostly US) and Tyverb (mostly Europe).” PMID 26571496 ↗ Nov 2015 “Lapatinib (Tykerb™) blocks signals that stimulate HER2-positive breast cancers to grow.” NCT00721630 ↗ “Lapatinib (also called Tyverb or Tykerb) will be compared with another drug trastuzumab” NCT01205217 ↗ “A Phase I Study of Lapatinib (Tykerb) Plus Ixabepilone (Ixempra)” NCT01454479 ↗ “Pazopanib Plus Paclitaxel (TAXOL) Plus Lapatinib (TYKERB)” NCT00388076 ↗ “Lapatinib (GW572016, Tykerb)” NCT01172223 ↗ |
| Known as | Tyverb | “Pilot Study of Lapatinib (Tyverb®) in Neoadjuvant Treatment for Patients With Locally Bladder Carcinoma Before Cystectomy” NCT01245660 ↗3“GlaxoSmithKline markets the drug lapatinib under the propriety names Tykerb (mostly US) and Tyverb (mostly Europe).” PMID 26571496 ↗ Nov 2015 “Lapatinib (also called Tyverb or Tykerb) will be compared with another drug trastuzumab” NCT01205217 ↗ “Lapatinib (Tyverb™)” NCT01495884 ↗ |
| Action | Inhibit | “dual kinase inhibitor” NCT00062686 ↗ |
| Modality | Small molecule | “Lapatinib is a small molecule, dual tyrosine kinase inhibitor” PMID 18188694 ↗ Jan 2008 |
| Route | Oral | “Oral Lapatinib” NCT00044343 ↗ |
| Target | EGFR | “dual tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor type 2 (HER2)” PMID 18188694 ↗ Jan 2008 |