Venetoclax

Short description: Medication

Venetoclax

Clinical data
Pronunciation| /vɛˈnɛtəklæks/
ve-NE-tə-klaks
Trade names| Venclexta, Venclyxto
Other names| GDC-0199, ABT-199, RG-7601
AHFS/Drugs.com| Monograph
MedlinePlus| a616028
License data|

* EU EMA: by INN
* US DailyMed: Venetoclax

Pregnancy
category|

* AU: C[1]

Routes of
administration| By mouth
ATC code|

* L01XX52 (WHO)

Legal status
Legal status|

* AU: S4 (Prescription only) [2][3]
* UK: POM (Prescription only) [4]
* US: ℞-only [5]
* EU: Rx-only [6]
* In general: ℞ (Prescription only)

Pharmacokinetic data
Protein binding| >99.9%[5]
Metabolism| Liver (CYP3A4, CYP3A5)
Elimination half-life| ~26 hours
Excretion| Feces (>99.9%; 20.8% as unchanged venetoclax)
Identifiers

IUPAC name

* 4-(4-{[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl}-1-piperazinyl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide

CAS Number|

* 1257044-40-8

PubChem CID|

* 49846579

DrugBank|

* DB11581

ChemSpider|

* 29315017

UNII|

* N54AIC43PW

KEGG|

* D10679

ChEBI|

* CHEBI:133021 Y

ChEMBL|

* ChEMBL3137309

PDB ligand|

* LBM (PDBe, RCSB PDB)

Chemical and physical data
Formula| C45H50ClN7O7S
Molar mass| 868.45 g·mol−1
3D model (JSmol)|

* Interactive image

SMILES

* CC1(CCC(=C(C1)c2ccc(cc2)Cl)CN3CCN(CC3)c4ccc(c(c4)Oc5cc6cc[nH]c6nc5)C(=O)NS(=O)(=O)c7ccc(c(c7)[N+](=O)[O-])NCC8CCOCC8)C

InChI

* InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54) COPY

* Key:LQBVNQSMGBZMKD-UHFFFAOYSA-N

Venetoclax, sold under the brand names Venclexta and Venclyxto, is a medication used to treat adults with chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), or acute myeloid leukemia (AML).[5][6]

The most common side effects are low levels of neutrophils (a type of white blood cell), diarrhea, nausea, anemia (low red blood cell counts), nose and throat infection and tiredness.[6]

Venetoclax attaches to a protein called Bcl-2.[6] This protein is present in high amounts in CLL cancer cells, where it helps the cells survive for longer in the body and makes them resistant to cancer medicines.[6] By attaching to Bcl-2 and blocking its actions, venetoclax causes the death of cancer cells and thereby slows down progression of the disease.[6]

## Contents

* 1 Medical uses
* 1.1 CLL/SLL
* 1.2 Other types of leukemia
* 2 Side effects
* 3 Pharmacology
* 3.1 Mechanism of action
* 3.2 Pharmacokinetics
* 4 History
* 5 Society and culture
* 6 Research
* 7 References
* 8 External links

## Medical uses

### CLL/SLL

In the US, venetoclax is indicated for adults with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).[5][7] Indication does not depend on mutation status (e. g. 17p deletion, IGHV mutation, 12+).

In the EU, venetoclax monotherapy is indicated for the treatment of chronic lymphocytic leukemia (CLL) in the presence of 17p deletion or TP53 mutation in adults who are unsuitable for or have failed a B cell receptor pathway inhibitor and for the treatment of CLL in the absence of 17p deletion or TP53 mutation in adults who have failed both chemoimmunotherapy and a B cell receptor pathway inhibitor.[6]

### Other types of leukemia

Venetoclax is also indicated as part of a combination therapy for acute myeloid leukemia (AML).[5] For this purpose it is used with azacitidine, decitabine, or low-dose cytarabine for newly diagnosed adults who are age 75 years or older, or those with other health problems where intensive chemotherapy cannot be used.[5]

## Side effects

Common side effects of venetoclax include neutropenia (low white blood cell count), nausea, anemia, diarrhea, upper respiratory tract infection, fatigue, and thrombocytopenia (low platelet count). Major side effects include tumor lysis syndrome and severe neutropenia. Additionally, this drug may cause fertility problems in males.[5]

## Pharmacology

### Mechanism of action

Venetoclax is a BH3-mimetic.[8] Venetoclax blocks the anti-apoptotic B-cell lymphoma-2 (Bcl-2) protein, leading to programmed cell death of CLL cells. Overexpression of Bcl-2 in some lymphoid malignancies has been linked to increased resistance to chemotherapy.[9]

### Pharmacokinetics

The maximum plasma concentration achieved after oral administration occurred 5–8 hours after dose.[5] Steady state maximum concentration with low-fat meal conditions at the 400 mg once daily dose was found to be 2.1 ± 1.1 μg/mL. It is recommended that venetoclax be administered with a meal.[5]

The apparent volume of distribution for venetoclax is approximately 256–321 L. It is highly bound to human plasma protein. Within a concentration range of 1-30 μM (0.87-26 μg/mL), the fraction unbound in plasma was less than 0.01.[5]

Venetoclax is metabolized by CYP3A4/5 as proven by in-vitro studies.[5] Those using the drug should not consume grapefruit products because they contain CYP3A inhibitors.[5] Additionally, while using venetoclax it is not recommended to use other drugs which contain CYP3A inhibitors (i.e.: erythromycin, ciprofloxacin, diltiazem, dronedarone, fluconazole, verapamil).[5] Venetoclax is excreted from the body via the fecal route.[5]

## History

In 2015, the United States Food and Drug Administration (FDA) granted the breakthrough therapy designation to venetoclax for people with CLL or SLL who have relapsed, become intolerant to, or refractory to previous treatment.

In April 2016, the FDA approved venetoclax for use in those with CLL who have 17p deletion (deletion located on the chromosome 17 short arm) and who have been treated with at least one prior therapy.[10][11][12][13] Based on overall response rate, the indication was approved under accelerated FDA approval.[5]

The efficacy of venetoclax was tested in a single-arm clinical trial of 106 participants with CLL who have a 17p deletion and who had received at least one prior therapy.[11] Trial participants took venetoclax orally every day, beginning with 20 mg and increasing over a five-week period to 400 mg.[11] Results showed that 80 percent of trial participants experienced a complete or partial remission of their cancer.[11] The trial was conducted in the US, Canada, France, Germany, Poland, the United Kingdom, and Australia.[13]

The application for venetoclax was granted priority review and accelerated approval along with breakthrough therapy designation and orphan drug designation.[11]

Venetoclax was approved for use in the European Union in December 2016.[6]

In June 2018, the FDA granted regular approval to venetoclax for people with CLL or small lymphocytic lymphoma (SLL), with or without 17p deletion, who have received at least one prior therapy.[14]

Approval was based on MURANO (NCT02005471), a randomized (1:1), multicenter, open-label trial of venetoclax with rituximab (VEN+R) versus bendamustine with rituximab (B+R) in 389 participants with CLL who had received at least one prior line of therapy.[14] Participants in the VEN+R arm completed a 5-week ramp-up venetoclax scheduleand then received venetoclax 400 mg once daily for 24 months measured from the rituximab start date.[14] Rituximab was initiated after venetoclax ramp-up and given for 6 cycles (375 mg/m2 intravenously on cycle 1 day 1 and 500 mg/m2 intravenously on day 1 of cycles 2–6, with a 28-day cycle length).[14] The comparator arm received 6 cycles of B+R (bendamustine 70 mg/m2 on days 1 and 2 of each 28-day cycle and rituximab at the above described dose and schedule).[14]

The application for venetoclax in combination with rituximab was granted priority review along with a breakthrough therapy designation.[14]

In November 2018, in the United States, venetoclax was approved in combination with azacitidine or decitabine or low-dose cytarabine for the treatment of newly diagnosed acute myeloid leukemia (AML) in adults who are age 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy.[15]

Accelerated approval was based on two open-label non-randomized trials in participants with newly diagnosed AML who were >= 75 years of age or had comorbidities that precluded the use of intensive induction chemotherapy.[15] Efficacy was established based on the rate of complete remission (CR) and CR duration.[15]

Study M14-358 (NCT02203773) was a non-randomized, open-label clinical trial of venetoclax in combination with azacitidine (n=67) or decitabine (n=13) in newly diagnosed participants with AML.[15] In combination with azacitidine, 25 participants achieved a CR (37%, 95% CI: 26, 50) with a median observed time in remission of 5.5 months (range: 0.4–30 months).[15] In combination with decitabine, 7 participants achieved a CR (54%, 95% CI: 25, 81) with a median observed time in remission of 4.7 months (range: 1.0–18 months).[15] The observed time in remission is the time from start of CR to data cut-off date or relapse from CR.[15] In a phase 3 study of azacitidine and venetoclax in untreated acute myeloid leukemia not eligible for standard induction chemotherapy, the addition of venetoclax to azacitidine resulted in an improvement in median overall survival (14.7 months versus 9.6 months) and improved complete remission rates.[16]

Study M14-387 (NCT02287233) was a non-randomized, open-label trial of venetoclax in combination with low-dose cytarabine (n=61) in newly diagnosed participants with AML, including participants with previous exposure to a hypomethylating agent for an antecedent hematologic disorder.[15] In combination with low-dose cytarabine, 13 participants achieved a CR (21%, 95% CI: 12, 34) with a median observed time in remission of 6 months (range: 0.03–25 months).[15]

In May 2019, the label was extended by accelerated approval to include all adults with CLL/SLL disregarding prior treatment or mutation status.[7]

Approval was based on CLL14 (NCT02242942), a randomized (1:1), multicenter, open label, actively controlled trial of venetoclax in combination with obinutuzumab (VEN+G) versus obinutuzumab in combination with chlorambucil (GClb) in 432 participants with previously untreated CLL with coexisting medical conditions.[7]

The major efficacy outcome was progression-free survival (PFS) assessed by an independent review committee.[7] The trial demonstrated a statistically significant improvement in PFS for participants who received VEN+G compared with those who received GClb (HR 0.33; 95% CI: 0.22, 0.51; p<0.0001).[7] Median PFS was not reached in either arm after a median follow-up duration of 28 months.[7] The overall response rate was 85% in VEN+G arm compared to 71% in GClb arm, p=0.0007.[7] The trial also demonstrated statistically significant improvements in rates of minimal residual disease negativity (less than one CLL cell per 104 leukocytes) in bone marrow and peripheral blood.[7] Overall survival data were not mature at this analysis.[7]

The FDA used the Real-Time Oncology Review and Assessment Aid Pilot Program for this application and granted priority review as well as orphan drug and breakthrough therapy designations.[7] Approval was granted 3.7 months ahead of the Prescription Drug User Fee Act (PDUFA) date.[7]

## Society and culture

AbbVie Inc. manufactures Venclexta.[11] It is marketed by both Abbvie and Genentech USA, which is a member of the Roche Group.[11] AbbVie and Genentech are both commercializing the drug within the United States, but only AbbVie has rights to do so outside of the U.S.[17]

According to Reuters 2016 Drugs to Watch, the 2020 forecast sales for venetoclax are US$1.48 billion.[18]: 3, 7–8 Competition as well as potential for combination is expected from other drugs such as ibrutinib and idelalisib, both of which were also approved in 2014 to treat CLL.[18]: 7–8 [19]

Venetoclax is patented by AbbVie Inc.[20][21][22][23]

## Research

As of 2016[update], venetoclax had been tested to treat other hematological cancers, including non-Hodgkin's lymphoma, multiple myeloma, diffuse large B-cell lymphoma and follicular lymphoma.[18]: 7–8

On 13 June 2020 at the European Hematology Association (EHA) annual congress, AbbVie and Roche announced the results of a Phase III trial that showed a 34 percent reduction in the risk of death in AML patients who were ineligible for intensive chemotherapy treated with venetoclax plus azacitidine compared to azacitidine plus placebo.[24][25][26] Several trials have assessed the combination of venetoclax with intensive chemotherapy in younger AML patients.[27]

## References

1. ↑ "Venetoclax (Venclexta) Use During Pregnancy". 29 May 2019. https://www.drugs.com/pregnancy/venetoclax.html.
2. ↑ "AusPAR: Venetoclax". 26 April 2022. https://www.tga.gov.au/auspar/auspar-venetoclax-2.
3. ↑ "Prescription medicines: registration of new chemical entities in Australia, 2017". 21 June 2022. https://www.tga.gov.au/resources/publication/publications/prescription-medicines-registration-new-chemical-entities-australia-2017.
4. ↑ "Venclyxto 10 mg film-coated tablets - Summary of Product Characteristics (SmPC)". 21 April 2020. https://www.medicines.org.uk/emc/product/2267/smpc.
5. ↑ 5.00 5.01 5.02 5.03 5.04 5.05 5.06 5.07 5.08 5.09 5.10 5.11 5.12 5.13 5.14 "Venclexta- venetoclax kit Venclexta- venetoclax tablet, film coated". 12 November 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b118a40d-6b56-cee3-10f6-ded821a97018.
6. ↑ 6.0 6.1 6.2 6.3 6.4 6.5 6.6 6.7 "Venclyxto EPAR". https://www.ema.europa.eu/en/medicines/human/EPAR/venclyxto. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
7. ↑ 7.00 7.01 7.02 7.03 7.04 7.05 7.06 7.07 7.08 7.09 7.10 "FDA approves venetoclax for CLL and SLL". U.S. Food and Drug Administration (FDA) (Press release). 15 May 2019. Retrieved 25 April 2020. This article incorporates text from this source, which is in the public domain.
8. ↑ "Targeting BCL2 With BH3 Mimetics: Basic Science and Clinical Application of Venetoclax in Chronic Lymphocytic Leukemia and Related B Cell Malignancies". Clinical Pharmacology and Therapeutics 101 (1): 89–98. January 2017. doi:10.1002/cpt.553. PMID 27806433.
9. ↑ "Center for Drug Evaluation and Research - Application 208573Orig1s000 - Division Director Summary Review". http://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208573Orig1s000SumR.pdf.
10. ↑ "Venclexta Tablets". 19 May 2016. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208573Orig1s000TOC.cfm.
11. ↑ 11.0 11.1 11.2 11.3 11.4 11.5 11.6 "FDA approves new drug for chronic lymphocytic leukemia in patients with a specific chromosomal abnormality". U.S. Food and Drug Administration (FDA) (Press release). 11 April 2016. Retrieved 25 April 2020. This article incorporates text from this source, which is in the public domain.
12. ↑ "Venetoclax (Venclexta) Tablets". 11 April 2016. https://www.fda.gov/drugs/resources-information-approved-drugs/venetoclax-venclexta-tablets. This article incorporates text from this source, which is in the public domain.
13. ↑ 13.0 13.1 "Drug Trials Snapshot: Venclexta". 11 April 2016. https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trials-snapshot-venclexta. This article incorporates text from this source, which is in the public domain.
14. ↑ 14.0 14.1 14.2 14.3 14.4 14.5 "FDA approves venetoclax for CLL or SLL, with or without 17p deletion, after one prior therapy". U.S. Food and Drug Administration (FDA) (Press release). 8 June 2018. Retrieved 25 April 2020. This article incorporates text from this source, which is in the public domain.
15. ↑ 15.0 15.1 15.2 15.3 15.4 15.5 15.6 15.7 15.8 "FDA approves venetoclax in combination for AML in adults". 21 November 2018. https://www.fda.gov/drugs/fda-approves-venetoclax-combination-aml-adults. This article incorporates text from this source, which is in the public domain.
16. ↑ "Azacitidine and Venetoclax in Previously Untreated Acute Myeloid Leukemia". The New England Journal of Medicine 383 (7): 617–629. August 2020. doi:10.1056/NEJMoa2012971. PMID 32786187.
17. ↑ "Inside the development of Venclexta, AbbVie's new leukemia drug". BioPharma Dive. http://www.biopharmadive.com/news/inside-the-development-of-venclexta-abbvies-new-leukemia-drug/417965/.
18. ↑ 18.0 18.1 18.2 "Drugs to Watch 2016 - Market Insight Report". Thomson Reuters. February 2016. http://images.info.science.thomsonreuters.biz/Web/ThomsonReutersScience/{7e677448-1313-40ae-9978-6be1a8532a08}_A4_MarketInsight_Report_0213_012__edits_2.pdf.
19. ↑ "Ibrutinib and Idelalisib Continue to Impress in CLL, May Eventually Replace Chemotherapy for Some Patients". OncLive. http://www.onclive.com/web-exclusives/ibrutinib-and-idelalisib-continue-to-impress-in-cll-may-eventually-replace-chemotherapy-for-some-patients.
20. ↑ "United States Patent: 9174982". http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=/netahtml/PTO/search-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=9,174,982&OS=9,174,982&RS=9,174,982.
21. ↑ "venetoclax". http://drugcentral.org/drugcard/5133.
22. ↑ "Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases - Patent US9174982 - PubChem". https://pubchem.ncbi.nlm.nih.gov/patent/US9174982#section=Patent-Identifier-Synonyms.
23. ↑ "Venetoclax | US Patents | Expiry | Expiration | Dates". https://www.pharmacompass.com/patent-expiry-expiration/venetoclax.
24. ↑ "BRIEF-Roche Reports Positive Phase 3 Results For Venclexta/Venclyxto Combination In Acute Myeloid Leukaemia". Reuters. 2020-06-13. https://uk.reuters.com/article/brief-roche-reports-positive-phase-3-res-idUKFWN2DQ02S.
25. ↑ "EHA: AbbVie, Roche cement Venclexta's place in AML with survival win". 13 June 2020. https://www.fiercepharma.com/pharma/eha-abbvie-roche-cement-venclexta-s-place-aml-survival-win.
26. ↑ "Venclexta/Venclyxto (venetoclax) Plus Azacitidine Demonstrates Statistically Significant Overall Survival Benefit and Improved Remission Rates in Treatment-Naïve Acute Myeloid Leukemia Patients". https://news.abbvie.com/news/press-releases/venclextavenclyxto-venetoclax-plus-azacitidine-demonstrates-statistically-significant-overall-survival-benefit-and-improved-remission-rates-in-treatment-nave-acute-myeloid-leukemia-patients.htm.
27. ↑ Molica, Matteo; Perrone, Salvatore; Federico, Vincenzo; Alati, Caterina; Molica, Stefano; Rossi, Marco (2023-12-22). "Venetoclax: A Game Changer in the Treatment of Younger AML Patients?" (in en). Cancers 16 (1): 73. doi:10.3390/cancers16010073. ISSN 2072-6694. PMID 38201501.

## External links

* "Venetoclax". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/venetoclax.
* "FDA In Brief: FDA warns about safety concerns related to investigational use of Venclexta (venetoclax) for multiple myeloma". 21 March 2019. https://www.fda.gov/news-events/fda-brief/fda-brief-fda-warns-about-safety-concerns-related-investigational-use-venclexta-venetoclax-multiple.
* "FDA Warns about the risks associated with the investigational use of Venclexta in Multiple Myeloma". 21 March 2019. https://www.fda.gov/drugs/drug-safety-and-availability/fda-warns-about-risks-associated-investigational-use-venclexta-multiple-myeloma.

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* Ceritinib
* Crizotinib

RET inhibitors: Vandetanib (also VEGFR and EGFR). Entrectinib (ALK, ROS1, NTRK). c-MET inhibitor: Cabozantinib (also VEGFR2).

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Non-receptor|

* bcr-abl
* Bosutinib
* Dasatinib
* Imatinib
* Nilotinib
* Ponatinib
* Radotinib

* Src (Bosutinib
* Dasatinib)

* Janus kinase
* Lestaurtinib
* Momelotinib
* Pacritinib
* Ruxolitinib

* MAP2K
* Binimetinib
* Cobimetinib
* Selumetinib
* Trametinib

* EML4-ALK
* Crizotinib
* Entrectinib
* Lorlatinib

* Bruton's
* Acalabrutinib
* Ibrutinib

Other|

* fusion protein against VEGF (Aflibercept)
* proapoptotic peptide against ANXA2 and prohibitin (Adipotide)
* exotoxin against IL-2 (Denileukin diftitox)
* mTOR inhibitors
* Everolimus
* Temsirolimus
* hedgehog inhibitors
* Sonidegib
* Vismodegib
* CDK inhibitor (Palbociclib
* Ribociclib)

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Original source: https://en.wikipedia.org/wiki/Venetoclax. Read more

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